| S7397 | Sorafenib | Sorafenib is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity. | 
                                                    
                                                        Mol Cancer, 2025, 24(1):34
                                                     
                                                    
                                                        Nat Commun, 2025, 16(1):509
                                                     
                                                    
                                                        Adv Sci (Weinh), 2025, 12(30):e04372
                                                     |   | 
                            
                                
                                    | S2475 | Imatinib | Imatinib is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy. | 
                                                    
                                                        Cancer Cell, 2025, 43(4):776-796.e14
                                                     
                                                    
                                                        Theranostics, 2025, 15(8):3589-3609
                                                     
                                                    
                                                        Genome Med, 2025, 17(1):14
                                                     |   | 
                            
                                
                                    | S1040 | Sorafenib tosylate | Sorafenib tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity. | 
                                                    
                                                        Int J Oncol, 2025, 67(3)72
                                                     
                                                    
                                                        Nature, 2024, 629(8013):927-936
                                                     
                                                    
                                                        Cell Mol Life Sci, 2024, 81(1):238
                                                     |   | 
                            
                                
                                    | S1026 | Imatinib Mesylate | Imatinib Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy. | 
                                                    
                                                        Sci Immunol, 2025, 10(109):eads5818
                                                     
                                                    
                                                        Blood Adv, 2025, bloodadvances.2024015364
                                                     
                                                    
                                                        Eur J Med Chem, 2025, 284:117211
                                                     |   | 
                            
                                
                                    | S7781 | Sunitinib | Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis. | 
                                                    
                                                        Cancer Cell, 2025, 43(4):776-796.e14
                                                     
                                                    
                                                        Mol Cancer, 2025, 24(1):179
                                                     
                                                    
                                                        Cells, 2025, 14(2)102
                                                     |   | 
                            
                                
                                    | S1490 | Ponatinib | Ponatinib is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy. | 
                                                    
                                                        Nat Commun, 2025, 16(1):471
                                                     
                                                    
                                                        Theranostics, 2025, 15(8):3589-3609
                                                     
                                                    
                                                        Virulence, 2025, 16(1):2489751
                                                     |   | 
                            
                                
                                    | S1178 | Regorafenib | Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces autophagy. | 
                                                    
                                                        Nat Commun, 2025, 16(1):509
                                                     
                                                    
                                                        Cell Death Differ, 2025, 10.1038/s41418-025-01536-1
                                                     
                                                    
                                                        Cell Mol Gastroenterol Hepatol, 2025, S2352-345X(25)00026-8
                                                     |   | 
                            
                                
                                    | S1005 | Axitinib | Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively. | 
                                                    
                                                        Cancer Cell, 2025, S1535-6108(25)00070-4
                                                     
                                                    
                                                        Chem Biol Interact, 2025, 418:111628
                                                     
                                                    
                                                        Development, 2025, 152(13)dev204684
                                                     |   | 
                            
                                
                                    | S1042 | Sunitinib malate | Sunitinib malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis. | 
                                                    
                                                        Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
                                                     
                                                    
                                                        iScience, 2024, 27(10):110862
                                                     
                                                    
                                                        Pharmaceuticals (Basel), 2024, 17(1)108
                                                     |   | 
                            
                                
                                    | S1010 | Nintedanib | Nintedanib is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3. | 
                                                    
                                                        Nat Commun, 2025, 16(1):471
                                                     
                                                    
                                                        Cell Death Dis, 2025, 16(1):196
                                                     
                                                    
                                                        Eur J Pharmacol, 2025, 1005:178058
                                                     |   | 
                            
                                
                                    | S1164 | Lenvatinib | Lenvatinib is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Lenvatinib (E7080) also inhibits FGFR1-4, PDGFR, Kit (c-Kit), RET (c-RET), and shows potent antitumor activities. Phase 3. | 
                                                    
                                                        Nature, 2025, 10.1038/s41586-025-08585-z
                                                     
                                                    
                                                        Drug Resist Updat, 2025, 81:101224
                                                     
                                                    
                                                        Nat Commun, 2025, 16(1):6451
                                                     |   | 
                            
                                
                                    | S2730 | Crenolanib | Crenolanib is a potent and selective inhibitor of PDGFRα/β with Kd of 2.1 nM/3.2 nM in CHO cells, also potently inhibits FLT3, sensitive to D842V mutation not V561D mutation, >100-fold more selective for PDGFR than c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, and Src. Crenolanib helps to induce mitophagy. | 
                                                    
                                                        Cancer Cell, 2025, S1535-6108(25)00070-4
                                                     
                                                    
                                                        Nat Commun, 2025, 16(1):1358
                                                     
                                                    
                                                        Cell Rep Med, 2025, S2666-3791(25)00102-8
                                                     |   | 
                            
                                
                                    | S1111 | Foretinib | Foretinib is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met (c-Met) and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2. | 
                                                    
                                                        J Microbiol, 2025, 63(2):e2409001
                                                     
                                                    
                                                        Int J Mol Sci, 2023, 24(1)757
                                                     
                                                    
                                                        Biol Open, 2023, 12(8)bio059994
                                                     |   | 
                            
                                
                                    | S3012 | Pazopanib | Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy. | 
                                                    
                                                        Nucleic Acids Res, 2025, 53(4)gkaf107
                                                     
                                                    
                                                        Commun Biol, 2025, 8(1):1185
                                                     
                                                    
                                                        Cell Rep Med, 2024, S2666-3791(24)00201-5
                                                     |   | 
                            
                                
                                    | S1017 | Cediranib (AZD2171) | Cediranib (AZD2171, NSC-732208) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Cediranib (AZD2171) induces autophagic vacuole accumulation. Phase 3. | 
                                                    
                                                        Front Oncol, 2024, 14:1302850
                                                     
                                                    
                                                        Cell Oncol (Dordr), 2023, 46(2):391-407
                                                     
                                                    
                                                        Cell Oncol (Dordr), 2023, 46(2):391-407
                                                     |   | 
                            
                                
                                    | S1035 | Pazopanib HCl | Pazopanib HCl is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death. | 
                                                    
                                                        iScience, 2024, 27(10):110862
                                                     
                                                    
                                                        iScience, 2023, 26(7):107116
                                                     
                                                    
                                                        NPJ Breast Cancer, 2022, 8(1):44
                                                     |   | 
                            
                                
                                    | S1018 | Dovitinib (TKI-258) | Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4. | 
                                                    
                                                        Spectrochim Acta A Mol Biomol Spectrosc, 2025, 343:126602
                                                     
                                                    
                                                        Biomed Pharmacother, 2024, 180:117533
                                                     
                                                    
                                                        Sci Rep, 2023, 13(1):20223
                                                     |   | 
                            
                                
                                    | S5077 | Regorafenib (BAY-734506) Monohydrate | Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga, regorafaenib monohydrate) Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively. | 
                                                    
                                                        Nature, 2024, 629(8011):450-457
                                                     
                                                    
                                                        iScience, 2024, 27(10):110862
                                                     
                                                    
                                                        STAR Protoc, 2024, 5(2):103090
                                                     |  | 
                            
                                
                                    | S1064 | Masitinib | Masitinib is a novel inhibitor for Kit (c-Kit) and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms. Phase 3. | 
                                                    
                                                        Cancer Res, 2025, 10.1158/0008-5472.CAN-24-2220
                                                     
                                                    
                                                        iScience, 2024, 27(10):110862
                                                     
                                                    
                                                        bioRxiv, 2024, 2023.11.21.568071
                                                     |   | 
                            
                                
                                    | S1207 | Tivozanib | Tivozanib is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 30 nM/6.5 nM/15 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met, EGFR and IGF-1R. Phase 3. | 
                                                    
                                                        bioRxiv, 2025, 2025.01.24.634732
                                                     
                                                    
                                                        Nat Commun, 2024, 15(1):4758
                                                     
                                                    
                                                        Nat Commun, 2024, 15(1):4758
                                                     |   | 
                            
                                
                                    | S8401 | Erdafitinib | Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis. | 
                                                    
                                                        Commun Biol, 2025, 8(1):394
                                                     
                                                    
                                                        Int J Mol Sci, 2025, 26(8)3525
                                                     
                                                    
                                                        J Clin Invest, 2024, 134(2)e169241
                                                     |   | 
                            
                                
                                    | S1003 | Linifanib (ABT-869) | Linifanib (ABT-869, AL39324, RG3635) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Linifanib (ABT-869) induces autophagy and apoptosis. Phase 3. | 
                                                    
                                                        Biomed Pharmacother, 2024, 180:117533
                                                     
                                                    
                                                        Cell Death Discov, 2023, 9(1):57
                                                     
                                                    
                                                        Cell Death Discov, 2023, 9(1):57
                                                     |   | 
                            
                                
                                    | S7765 | Dovitinib (TKI258) Lactate monohydrate | Dovitinib (TKI258) Lactate monohydrate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4. | 
                                                    
                                                        Mol Cell, 2021, S1097-2765(21)00507-4
                                                     
                                                    
                                                        Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
                                                     
                                                    
                                                        Cancer Res, 2021, canres.1780.2020
                                                     |   | 
                            
                                
                                    | S5240 | Lenvatinib Mesylate | Lenvatinib Mesylate is a synthetic, orally available tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR1-3), fibroblast growth factor receptor (FGFR1-4), platelet-derived growth factor receptor α (PDGFRα), stem cell factor receptor (Kit (c-Kit)), and rearranged during transfection (RET (c-RET)). Lenvatinib Mesylate has potential antineoplastic activity. | 
                                                    
                                                        Nat Commun, 2024, 15(1):1754
                                                     
                                                    
                                                        iScience, 2024, 27(10):110862
                                                     
                                                    
                                                        J Hepatocell Carcinoma, 2023, 10:697-712
                                                     |  | 
                            
                                
                                    | S1536 | CP-673451 | CP-673451 is a selective inhibitor of PDGFRα/β with IC50 of 10 nM/1 nM in cell-free assays, exhibits >450-fold selectivity over other angiogenic receptors, has antiangiogenic and antitumor activity. | 
                                                    
                                                        Cancer Res, 2025, 10.1158/0008-5472.CAN-24-2220
                                                     
                                                    
                                                        Cell Rep Med, 2024, S2666-3791(24)00201-5
                                                     
                                                    
                                                        Cancer Lett, 2024, 604:217219
                                                     |   | 
                            
                                
                                    | S1470 | Orantinib (SU6668) | Orantinib (TSU-68, SU6668) has greatest potency against PDGFR autophosphorylation with Ki of 8 nM in a cell-free assay, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit EGFR. Phase 3. | 
                                                    
                                                        bioRxiv, 2023, 2023.05.11.540170
                                                     
                                                    
                                                        bioRxiv, 2023, 2023.05.11.540170
                                                     
                                                    
                                                        J Pers Med, 2022, 12(2)258
                                                     |   | 
                            
                                
                                    | S4947 | Regorafenib Hydrochloride | Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM, 4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. | 
                                                    
                                                        Cancers (Basel), 2023, 15(18)4477
                                                     
                                                    
                                                        Cancers (Basel), 2023, 15(18)4477
                                                     
                                                    
                                                        J Clin Med, 2023, 12(23)7267
                                                     |  | 
                            
                                
                                    | S1363 | Ki8751 | Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR. | 
                                                    
                                                        Elife, 2025, 13RP98612
                                                     
                                                    
                                                        Nat Commun, 2024, 15(1):2539
                                                     
                                                    
                                                        Drug Des Devel Ther, 2023, 17:1567-1582
                                                     |   | 
                            
                                
                                    | S1244 | Amuvatinib (MP-470) | Amuvatinib (MP-470, HPK 56) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Amuvatinib suppresses c-MET and c-RET. Amuvatinib is also active as a DNA repair protein Rad51 inhibitor with antineoplastic activity. Phase 2. | 
                                                    
                                                        Cancer Res, 2025, 10.1158/0008-5472.CAN-24-2220
                                                     
                                                    
                                                        bioRxiv, 2024, 2023.11.21.568071
                                                     
                                                    
                                                        Microbiol Spectr, 2023, e0510522.
                                                     |   | 
                            
                                
                                    | S5234 | Nintedanib Ethanesulfonate Salt | Nintedanib (Intedanib, BIBF 1120) is a small molecule tyrosine-kinase inhibitor with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β, respectively. | 
                                                    
                                                        iScience, 2024, 27(10):110862
                                                     
                                                    
                                                        Am J Cancer Res, 2023, 13(2):355-378
                                                     
                                                    
                                                        Theranostics, 2022, 12(2):747-766
                                                     |  | 
                            
                                
                                    | S7667 | SU5402 | SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively. | 
                                                    
                                                        Int J Mol Sci, 2025, 26(8)3536
                                                     
                                                    
                                                        Basic Clin Pharmacol Toxicol, 2025, 136(5):e70022
                                                     
                                                    
                                                        Sci Adv, 2025, 11(30):eadi2370
                                                     |   | 
                            
                                
                                    | S8024 | Tyrphostin AG 1296 | Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR. Tyrphostin AG1296 inhibits FGFR and c-Kit with IC50 of 12.3 μM and 1.8 μM in Swiss 3T3 cells. Tyrphostin AG1296 induces dramatic apoptosis in A375R cells. | 
                                                    
                                                        Dev Cell, 2022, 57(12):1466-1481.e6
                                                     
                                                    
                                                        Front Pharmacol, 2021, 12:804327
                                                     
                                                    
                                                        Mol Med Rep, 2021, 23(4):1
                                                     |   | 
                            
                                
                                    | S1032 | Motesanib Diphosphate (AMG-706) | Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit (c-Kit), ~10-fold more selective for VEGFR than PDGFR and Ret. Phase 3. | 
                                                    
                                                        Front Cell Dev Biol, 2022, 10:836179
                                                     
                                                    
                                                        J Pharm Sci, 2022, 111(8):2180-2190
                                                     
                                                    
                                                        Drug Metab Dispos, 2021, 49(1):53-61
                                                     |   | 
                            
                                
                                    | S8553 | Avapritinib | Avapritinib is a small molecule kinase inhibitor that potently inhibits PDGFRα D842V mutant activity in vitro (IC50 = 0.5 nM) and PDGFRα D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogous Kit (c-Kit) mutation, D816V in Kit (c-Kit) Exon 17 (IC50 = 0.5 nM). | 
                                                    
                                                        Cancer Cell, 2025, S1535-6108(25)00070-4
                                                     
                                                    
                                                        Sci Rep, 2024, 14(1):7204
                                                     
                                                    
                                                        Curr Drug Metab, 2024, 25(3):197-204
                                                     |  | 
                            
                                
                                    | S1181 | ENMD-2076 | ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2. | 
                                                    
                                                        Int J Biol Macromol, 2025, 292:139119
                                                     
                                                    
                                                        Cell, 2021, 184(2):334-351.e20
                                                     
                                                    
                                                        Sci Adv, 2021, 7(4)eabd7851
                                                     |   | 
                            
                                
                                    | S4736 | Trapidil | Trapidil (Rocornal, Trapymin, Avantrin, Trapymine) is a PDGF antagonist that can inhibit the proliferation of the PDGF-producing glioma cells. | 
                                                    
                                                        J Immunother Cancer, 2024, 12(11)e009805
                                                     
                                                    
                                                        J Pers Med, 2022, 12(2)258
                                                     
                                                    
                                                        Hum Cell, 2022, 10.1007/s13577-022-00671-y
                                                     |  | 
                            
                                
                                    | S8757 | Ripretinib | Ripretinib is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of the tumor-associated antigens (TAA) mast/stem cell factor receptor (SCFR) Kit (c-Kit) and PDGFR-alpha, with IC50 values of 4 nM, 8 nM, 18 nM, 5 nM and 14 nM for WT Kit (c-Kit), V654A Kit (c-Kit), T670I Kit (c-Kit), D816H Kit (c-Kit) and D816V Kit (c-Kit), respectively. | 
                                                    
                                                        Nature, 2024, 629(8011):450-457
                                                     
                                                    
                                                        Nature, 2024, 629(8011):450-457
                                                     
                                                    
                                                        Cell Rep Med, 2024, S2666-3791(24)00201-5
                                                     |  | 
                            
                                
                                    | S2622 | PP121 | PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM. | 
                                                    
                                                        Life Sci Alliance, 2021, 4(2)e202000882
                                                     
                                                    
                                                        PLoS One, 2016, 11(10):e0164895
                                                     
                                                    
                                                        PLoS One, 2016, 11(10):e0164895
                                                     |   | 
                            
                                
                                    | S8015 | Agerafenib (CEP-32496) | Agerafenib (CEP-32496) is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret (c-Ret), PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2. | 
                                                    
                                                        Mol Pharmacol, 2021, 99(6):435-447
                                                     
                                                    
                                                        Dis Model Mech, 2020, dmm.047779
                                                     
                                                    
                                                        Cancer Immunol Res, 2019, 
                                                     |  | 
                            
                                
                                    | S2231 | Telatinib | Telatinib (BAY 57-9352) is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively. Phase 2. | 
                                                    
                                                        Sci Adv, 2022, 8(6):eabg9455
                                                     
                                                    
                                                        Leiden University Scholarly Publications, 2020, N/A
                                                     
                                                    
                                                        Cell Stem Cell, 2019, 24(4):654-669
                                                     |   | 
                            
                                
                                    | S2774 | MK-2461 | MK-2461 is a potent, multi-targeted inhibitor for c-Met(WT/mutants) with IC50 of 0.4-2.5 nM, less potent to Ron, Flt1; 8- to 30-fold greater selectivity of c-Met targets versus FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB. Phase 1/2. | 
                                                    
                                                        Mol Carcinog, 2021, 60(7):481-496
                                                     
                                                    
                                                        G3 (Bethesda), 2021, 11(10)jkab265
                                                     
                                                    
                                                        Mol Cell Biochem, 2018, 449(1-2):1-8
                                                     |   | 
                            
                                
                                    | S7003 | AZD2932 | AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively. | 
                                                    
                                                        Cancer Res, 2020, canres.1992.2020
                                                     
                                                    
                                                        Molecules, 2020, 8;25(9) pii: E2220
                                                     
                                                    
                                                        Development, 2016, 143(23):4394-4404
                                                     |  | 
                            
                                
                                    | S0504 | SU14813 | SU14813 (SU 014813) is a multiple receptor tyrosine kinase inhibitor with IC50 of 50 nM, 2 nM, 4 nM and 15 nM for VEGFR2, VEGFR1, PDGFRβ and Kit (c-Kit). SU14813 exhibits potent antiangiogenic and antitumor activity. | 
                                                    
                                                        Cancer Cell, 2022, S1535-6108(22)00312-9
                                                     
                                                    
                                                        Adv Sci (Weinh), 2021, e2101848
                                                     |  | 
                            
                                
                                    | S8721 | PDGFR inhibitor 1 | PDGFR inhibitor 1 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of Kit (c-Kit) and PDGFR with potential antineoplastic activity. It also inhibits several other kinases, including VEGFR2, TIE2, PDGFR-beta and CSF1R, thereby further inhibiting tumor cell growth. | 
                                                    
                                                        bioRxiv, 2025, 2025.06.11.659120
                                                     
                                                    
                                                        Elife, 2023, 12e79840
                                                     
                                                    
                                                        Elife, 2023, 12e79840
                                                     |  | 
                            
                                
                                    | S6526 | SKLB 610 | SKLB-610 is a multi-target inhibitor of the tyrosine kinases. It is most potent against VEGFR2 and exhibits slightly weaker inhibitor of FGFR2 and PDGFR. | 
                                                    
                                                        Biomed Pharmacother, 2022, 149:112922
                                                     
                                                    
                                                        Int J Mol Sci, 2022, 23(14)7853
                                                     |  | 
                            
                                
                                    | S8161 | ON123300 | ON123300 is a potent and multi-targeted kinase inhibitor with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM for CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), and Fyn, respectively. | 
                                                    
                                                        Cell Rep Med, 2025, S2666-3791(25)00231-9
                                                     
                                                    
                                                        Cell Rep, 2024, 43(7):114446
                                                     
                                                    
                                                        J Cell Sci, 2021, jcs.258685
                                                     |  | 
                            
                                
                                    | S2895 | Tyrphostin 9 | Tyrphostin 9 (SF 6847, RG-50872) is firstly designed as an EGFR inhibitor with IC50 of 460 μM, but is also found to be more potent to PDGFR with IC50 of 0.5 μM. | 
                                                    
                                                        Cell Rep, 2022, 38(10):110475
                                                     |  | 
                            
                                
                                    | F1540 | PDGFR α/β Antibody [C19P10] |  |  |  | 
                            
                                
                                    | F1500New | Phospho-PDGF Receptor β (Tyr740) Antibody [M18D12] |  |  |  | 
                            
                                
                                    | E4449 | AG 825 | AG-825 (Tyrphostin AG-825) is a potent and selective inhibitor of ErbB2 with IC50 values of 0.15 µM. It also inhibits  PDGFR autophosphorylation with IC50 value of 40 µM. It exhibits anti-cancer activity and significantly induces apoptosis in cancer cells. |  |  | 
                            
                                
                                    | A2378 | Rinucumab (Anti-PDGFRB / CD140b) | Rinucumab (Anti-PDGFRB / CD140b) is an anti-platelet-derived growth factor receptor beta (anti-PDGFR-beta) monoclonal antibody and has a potential to study neovascular age-related macular degeneration. MW: 145.5 kD. |  |  | 
                            
                                
                                    | A2379 | Olaratumab (Anti-PDGFRA / CD140a) | Olaratumab (IMC-3G3; LY3012207) is a fully human IgG1 monoclonal antibody directed against the platelet-derived growth factor receptor alpha (PDGFR alpha) with potential antineoplastic activity. MW: 145.5 kD. | 
                                                    
                                                        Nat Commun, 2025, 16(1):471
                                                     |  | 
                            
                                
                                    | S7688 | Ki20227 | Ki20227 is an orally active and highly selective inhibitor of c-Fms tyrosine kinase(CSF1R) with IC50 of 2 nM, 12 nM, 451 nM and 217 nM for c-Fms, vascular endothelial growth factor receptor-2 (KDR/VEGFR-2), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor beta (PDGFRβ), respectively. | 
                                                    
                                                        Cancer Immunol Immunother, 2024, 73(5):76
                                                     
                                                    
                                                        Cancer Immunol Immunother, 2024, 73(5):76
                                                     |  | 
                            
                                
                                    | S5272 | Toceranib phosphate | Toceranib phosphate (Palladia, SU11654), the phosphate salt of toceranib, is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR, and Kit with Ki values of 6 nM and 5 nM for Flk-1/KDR and PDGFRβ, respectively. | 
                                                    
                                                        Front Vet Sci, 2024, 11:1392728
                                                     |  | 
                            
                                
                                    | S4018 | Sennoside B | Sennoside B, a kind of irritant laxative isolated from rhei rhizome, inhibits PDGF-stimulated cell proliferation. |  |  | 
                            
                                
                                    | F1260New | Phospho-PDGF Receptor β (Tyr1021) Antibody [M20P20] |  |  |  | 
                            
                                
                                    | S0763 | Tyrphostin AG1433 | Tyrphostin AG1433 (AG1433, SU1433) is a selective platelet-derived growth factor receptor β (PDGFRβ) and vascular endothelial growth factor receptor 2 (VEGFR-2, Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively. |  |  | 
                            
                                
                                    | E0616 | Chiauranib | Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy. |  |  | 
                            
                                
                                    | E2828New | AG 1295 | AG 1295 is a selective and specific inhibitor of platelet-derived growth factor receptor (PDGFR) tyrosine-kinase. It inhibits PDGFR autophosphorylation with IC50 values of 0.3-0.5 μM in membrane autophosphorylation assays, respectively. |  |  | 
                            
                                
                                    | S6843 | Vorolanib | Vorolanib (X-82,CM082) is an oral, multikinase, dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with antiangiogenic and antineoplastic activities. |  |  | 
                            
                                
                                    | A2684 | Anti-PDGFC / VEGFE | Anti-PDGFC / VEGFE is a monoclonal antibody targeting PDGF-CC. It can be used in the research of cancer, fibrosis and neuropathologies. MW :145.9 KD. |  |  | 
                            
                                
                                    | E0814 | Masitinib mesylate | Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit with IC50 of 200 nM for human recombinant c-Kit, also inhibits PDGFRα/β with IC50s of 540/800 nM, Lyn with IC50 of 510 nM for LynB, and, to a lesser extent, FGFR3 and FAK. |  |  | 
                            
                                
                                    | S8780 | AZD3229 | AZD3229 is a potent, pan-Kit (c-Kit) mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant Kit (c-Kit) driven Ba/F3 cell lines (GI50=1-50 nM), with good margin to KDR-driven effects. It also inhibits PDGFR mutants (Tel-PDGFRα, Tel-PDGFRβ, V561D/D842V). |  |  | 
                            
                                
                                    | E2548 | N-(p-Coumaroyl) Serotonin | N-(p-Coumaroyl) Serotonin (p-coumaroylserotonin) is a polyphenol isolated from the seeds of safflower and has antioxidative, anti-atherogenic and anti-inflammatory properties, can inhibits PDGF-induced on phosphorylation of PDGF receptor and Ca2+ release from sarcoplasmic reticulum. |  |  | 
                            
                                
                                    | E0050 | Seralutinib (GB002) | Seralutinib (PK10571, GB002) is a novel PDGFR kinase inhibitor with IC50s of 8 nM and 10 nM for PDGFRα and PDGFRβ in enzyme assays, respectively. |  |  | 
                            
                                
                                    | E2393 | JNJ-10198409 | JNJ-10198409, a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor with IC50 of 2 nM, is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent, has good activity against PDGFRβ kinase and PDGFRα kinase with IC50 of 4.2 and 45 nM, respectively. |  |  | 
                            
                                
                                    | F1497New | Phospho-PDGF Receptor β (Tyr771) Antibody [C22C4] |  |  |  | 
                            
                                
                                    | S9973 | Flumatinib (HH-GV-678) | Flumatinib (HH-GV-678) is a novel inhibitor of Bcr-Abl with IC50 values of 1.2  nM, 307.6  nM and 665.5  nM for c-Abl, PDGFRβand c-Kit, respectively. |  |  | 
                            
                                
                                    | F0804New | Phospho-PDGF Receptor β (Tyr1009) Antibody [G5H10] |  |  |  | 
                            
                        
                    
                    
                        
                        
                            
                        
                            
                                
                                    
                                        | S7397 | Sorafenib | Sorafenib is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity. | 
                                                        Mol Cancer, 2025, 24(1):34 
                                                        Nat Commun, 2025, 16(1):509 
                                                        Adv Sci (Weinh), 2025, 12(30):e04372 |   | 
                                
                                    
                                        | S2475 | Imatinib | Imatinib is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy. | 
                                                        Cancer Cell, 2025, 43(4):776-796.e14 
                                                        Theranostics, 2025, 15(8):3589-3609 
                                                        Genome Med, 2025, 17(1):14 |   | 
                                
                                    
                                        | S1040 | Sorafenib tosylate | Sorafenib tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity. | 
                                                        Int J Oncol, 2025, 67(3)72 
                                                        Nature, 2024, 629(8013):927-936 
                                                        Cell Mol Life Sci, 2024, 81(1):238 |   | 
                                
                                    
                                        | S1026 | Imatinib Mesylate | Imatinib Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy. | 
                                                        Sci Immunol, 2025, 10(109):eads5818 
                                                        Blood Adv, 2025, bloodadvances.2024015364 
                                                        Eur J Med Chem, 2025, 284:117211 |   | 
                                
                                    
                                        | S7781 | Sunitinib | Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis. | 
                                                        Cancer Cell, 2025, 43(4):776-796.e14 
                                                        Mol Cancer, 2025, 24(1):179 
                                                        Cells, 2025, 14(2)102 |   | 
                                
                                    
                                        | S1490 | Ponatinib | Ponatinib is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy. | 
                                                        Nat Commun, 2025, 16(1):471 
                                                        Theranostics, 2025, 15(8):3589-3609 
                                                        Virulence, 2025, 16(1):2489751 |   | 
                                
                                    
                                        | S1178 | Regorafenib | Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces autophagy. | 
                                                        Nat Commun, 2025, 16(1):509 
                                                        Cell Death Differ, 2025, 10.1038/s41418-025-01536-1 
                                                        Cell Mol Gastroenterol Hepatol, 2025, S2352-345X(25)00026-8 |   | 
                                
                                    
                                        | S1005 | Axitinib | Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively. | 
                                                        Cancer Cell, 2025, S1535-6108(25)00070-4 
                                                        Chem Biol Interact, 2025, 418:111628 
                                                        Development, 2025, 152(13)dev204684 |   | 
                                
                                    
                                        | S1042 | Sunitinib malate | Sunitinib malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis. | 
                                                        Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5 
                                                        iScience, 2024, 27(10):110862 
                                                        Pharmaceuticals (Basel), 2024, 17(1)108 |   | 
                                
                                    
                                        | S1010 | Nintedanib | Nintedanib is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3. | 
                                                        Nat Commun, 2025, 16(1):471 
                                                        Cell Death Dis, 2025, 16(1):196 
                                                        Eur J Pharmacol, 2025, 1005:178058 |   | 
                                
                                    
                                        | S1164 | Lenvatinib | Lenvatinib is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Lenvatinib (E7080) also inhibits FGFR1-4, PDGFR, Kit (c-Kit), RET (c-RET), and shows potent antitumor activities. Phase 3. | 
                                                        Nature, 2025, 10.1038/s41586-025-08585-z 
                                                        Drug Resist Updat, 2025, 81:101224 
                                                        Nat Commun, 2025, 16(1):6451 |   | 
                                
                                    
                                        | S2730 | Crenolanib | Crenolanib is a potent and selective inhibitor of PDGFRα/β with Kd of 2.1 nM/3.2 nM in CHO cells, also potently inhibits FLT3, sensitive to D842V mutation not V561D mutation, >100-fold more selective for PDGFR than c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, and Src. Crenolanib helps to induce mitophagy. | 
                                                        Cancer Cell, 2025, S1535-6108(25)00070-4 
                                                        Nat Commun, 2025, 16(1):1358 
                                                        Cell Rep Med, 2025, S2666-3791(25)00102-8 |   | 
                                
                                    
                                        | S1111 | Foretinib | Foretinib is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met (c-Met) and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2. | 
                                                        J Microbiol, 2025, 63(2):e2409001 
                                                        Int J Mol Sci, 2023, 24(1)757 
                                                        Biol Open, 2023, 12(8)bio059994 |   | 
                                
                                    
                                        | S3012 | Pazopanib | Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy. | 
                                                        Nucleic Acids Res, 2025, 53(4)gkaf107 
                                                        Commun Biol, 2025, 8(1):1185 
                                                        Cell Rep Med, 2024, S2666-3791(24)00201-5 |   | 
                                
                                    
                                        | S1017 | Cediranib (AZD2171) | Cediranib (AZD2171, NSC-732208) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Cediranib (AZD2171) induces autophagic vacuole accumulation. Phase 3. | 
                                                        Front Oncol, 2024, 14:1302850 
                                                        Cell Oncol (Dordr), 2023, 46(2):391-407 
                                                        Cell Oncol (Dordr), 2023, 46(2):391-407 |   | 
                                
                                    
                                        | S1035 | Pazopanib HCl | Pazopanib HCl is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death. | 
                                                        iScience, 2024, 27(10):110862 
                                                        iScience, 2023, 26(7):107116 
                                                        NPJ Breast Cancer, 2022, 8(1):44 |   | 
                                
                                    
                                        | S1018 | Dovitinib (TKI-258) | Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4. | 
                                                        Spectrochim Acta A Mol Biomol Spectrosc, 2025, 343:126602 
                                                        Biomed Pharmacother, 2024, 180:117533 
                                                        Sci Rep, 2023, 13(1):20223 |   | 
                                
                                    
                                        | S5077 | Regorafenib (BAY-734506) Monohydrate | Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga, regorafaenib monohydrate) Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively. | 
                                                        Nature, 2024, 629(8011):450-457 
                                                        iScience, 2024, 27(10):110862 
                                                        STAR Protoc, 2024, 5(2):103090 |  | 
                                
                                    
                                        | S1064 | Masitinib | Masitinib is a novel inhibitor for Kit (c-Kit) and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms. Phase 3. | 
                                                        Cancer Res, 2025, 10.1158/0008-5472.CAN-24-2220 
                                                        iScience, 2024, 27(10):110862 
                                                        bioRxiv, 2024, 2023.11.21.568071 |   | 
                                
                                    
                                        | S1207 | Tivozanib | Tivozanib is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 30 nM/6.5 nM/15 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met, EGFR and IGF-1R. Phase 3. | 
                                                        bioRxiv, 2025, 2025.01.24.634732 
                                                        Nat Commun, 2024, 15(1):4758 
                                                        Nat Commun, 2024, 15(1):4758 |   | 
                                
                                    
                                        | S8401 | Erdafitinib | Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis. | 
                                                        Commun Biol, 2025, 8(1):394 
                                                        Int J Mol Sci, 2025, 26(8)3525 
                                                        J Clin Invest, 2024, 134(2)e169241 |   | 
                                
                                    
                                        | S1003 | Linifanib (ABT-869) | Linifanib (ABT-869, AL39324, RG3635) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Linifanib (ABT-869) induces autophagy and apoptosis. Phase 3. | 
                                                        Biomed Pharmacother, 2024, 180:117533 
                                                        Cell Death Discov, 2023, 9(1):57 
                                                        Cell Death Discov, 2023, 9(1):57 |   | 
                                
                                    
                                        | S7765 | Dovitinib (TKI258) Lactate monohydrate | Dovitinib (TKI258) Lactate monohydrate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4. | 
                                                        Mol Cell, 2021, S1097-2765(21)00507-4 
                                                        Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x 
                                                        Cancer Res, 2021, canres.1780.2020 |   | 
                                
                                    
                                        | S5240 | Lenvatinib Mesylate | Lenvatinib Mesylate is a synthetic, orally available tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR1-3), fibroblast growth factor receptor (FGFR1-4), platelet-derived growth factor receptor α (PDGFRα), stem cell factor receptor (Kit (c-Kit)), and rearranged during transfection (RET (c-RET)). Lenvatinib Mesylate has potential antineoplastic activity. | 
                                                        Nat Commun, 2024, 15(1):1754 
                                                        iScience, 2024, 27(10):110862 
                                                        J Hepatocell Carcinoma, 2023, 10:697-712 |  | 
                                
                                    
                                        | S1536 | CP-673451 | CP-673451 is a selective inhibitor of PDGFRα/β with IC50 of 10 nM/1 nM in cell-free assays, exhibits >450-fold selectivity over other angiogenic receptors, has antiangiogenic and antitumor activity. | 
                                                        Cancer Res, 2025, 10.1158/0008-5472.CAN-24-2220 
                                                        Cell Rep Med, 2024, S2666-3791(24)00201-5 
                                                        Cancer Lett, 2024, 604:217219 |   | 
                                
                                    
                                        | S1470 | Orantinib (SU6668) | Orantinib (TSU-68, SU6668) has greatest potency against PDGFR autophosphorylation with Ki of 8 nM in a cell-free assay, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit EGFR. Phase 3. | 
                                                        bioRxiv, 2023, 2023.05.11.540170 
                                                        bioRxiv, 2023, 2023.05.11.540170 
                                                        J Pers Med, 2022, 12(2)258 |   | 
                                
                                    
                                        | S4947 | Regorafenib Hydrochloride | Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM, 4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. | 
                                                        Cancers (Basel), 2023, 15(18)4477 
                                                        Cancers (Basel), 2023, 15(18)4477 
                                                        J Clin Med, 2023, 12(23)7267 |  | 
                                
                                    
                                        | S1363 | Ki8751 | Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR. | 
                                                        Elife, 2025, 13RP98612 
                                                        Nat Commun, 2024, 15(1):2539 
                                                        Drug Des Devel Ther, 2023, 17:1567-1582 |   | 
                                
                                    
                                        | S1244 | Amuvatinib (MP-470) | Amuvatinib (MP-470, HPK 56) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Amuvatinib suppresses c-MET and c-RET. Amuvatinib is also active as a DNA repair protein Rad51 inhibitor with antineoplastic activity. Phase 2. | 
                                                        Cancer Res, 2025, 10.1158/0008-5472.CAN-24-2220 
                                                        bioRxiv, 2024, 2023.11.21.568071 
                                                        Microbiol Spectr, 2023, e0510522. |   | 
                                
                                    
                                        | S5234 | Nintedanib Ethanesulfonate Salt | Nintedanib (Intedanib, BIBF 1120) is a small molecule tyrosine-kinase inhibitor with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β, respectively. | 
                                                        iScience, 2024, 27(10):110862 
                                                        Am J Cancer Res, 2023, 13(2):355-378 
                                                        Theranostics, 2022, 12(2):747-766 |  | 
                                
                                    
                                        | S7667 | SU5402 | SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively. | 
                                                        Int J Mol Sci, 2025, 26(8)3536 
                                                        Basic Clin Pharmacol Toxicol, 2025, 136(5):e70022 
                                                        Sci Adv, 2025, 11(30):eadi2370 |   | 
                                
                                    
                                        | S8024 | Tyrphostin AG 1296 | Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR. Tyrphostin AG1296 inhibits FGFR and c-Kit with IC50 of 12.3 μM and 1.8 μM in Swiss 3T3 cells. Tyrphostin AG1296 induces dramatic apoptosis in A375R cells. | 
                                                        Dev Cell, 2022, 57(12):1466-1481.e6 
                                                        Front Pharmacol, 2021, 12:804327 
                                                        Mol Med Rep, 2021, 23(4):1 |   | 
                                
                                    
                                        | S1032 | Motesanib Diphosphate (AMG-706) | Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit (c-Kit), ~10-fold more selective for VEGFR than PDGFR and Ret. Phase 3. | 
                                                        Front Cell Dev Biol, 2022, 10:836179 
                                                        J Pharm Sci, 2022, 111(8):2180-2190 
                                                        Drug Metab Dispos, 2021, 49(1):53-61 |   | 
                                
                                    
                                        | S8553 | Avapritinib | Avapritinib is a small molecule kinase inhibitor that potently inhibits PDGFRα D842V mutant activity in vitro (IC50 = 0.5 nM) and PDGFRα D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogous Kit (c-Kit) mutation, D816V in Kit (c-Kit) Exon 17 (IC50 = 0.5 nM). | 
                                                        Cancer Cell, 2025, S1535-6108(25)00070-4 
                                                        Sci Rep, 2024, 14(1):7204 
                                                        Curr Drug Metab, 2024, 25(3):197-204 |  | 
                                
                                    
                                        | S1181 | ENMD-2076 | ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2. | 
                                                        Int J Biol Macromol, 2025, 292:139119 
                                                        Cell, 2021, 184(2):334-351.e20 
                                                        Sci Adv, 2021, 7(4)eabd7851 |   | 
                                
                                    
                                        | S8757 | Ripretinib | Ripretinib is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of the tumor-associated antigens (TAA) mast/stem cell factor receptor (SCFR) Kit (c-Kit) and PDGFR-alpha, with IC50 values of 4 nM, 8 nM, 18 nM, 5 nM and 14 nM for WT Kit (c-Kit), V654A Kit (c-Kit), T670I Kit (c-Kit), D816H Kit (c-Kit) and D816V Kit (c-Kit), respectively. | 
                                                        Nature, 2024, 629(8011):450-457 
                                                        Nature, 2024, 629(8011):450-457 
                                                        Cell Rep Med, 2024, S2666-3791(24)00201-5 |  | 
                                
                                    
                                        | S2622 | PP121 | PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM. | 
                                                        Life Sci Alliance, 2021, 4(2)e202000882 
                                                        PLoS One, 2016, 11(10):e0164895 
                                                        PLoS One, 2016, 11(10):e0164895 |   | 
                                
                                    
                                        | S8015 | Agerafenib (CEP-32496) | Agerafenib (CEP-32496) is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret (c-Ret), PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2. | 
                                                        Mol Pharmacol, 2021, 99(6):435-447 
                                                        Dis Model Mech, 2020, dmm.047779 
                                                        Cancer Immunol Res, 2019,  |  | 
                                
                                    
                                        | S2231 | Telatinib | Telatinib (BAY 57-9352) is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively. Phase 2. | 
                                                        Sci Adv, 2022, 8(6):eabg9455 
                                                        Leiden University Scholarly Publications, 2020, N/A 
                                                        Cell Stem Cell, 2019, 24(4):654-669 |   | 
                                
                                    
                                        | S2774 | MK-2461 | MK-2461 is a potent, multi-targeted inhibitor for c-Met(WT/mutants) with IC50 of 0.4-2.5 nM, less potent to Ron, Flt1; 8- to 30-fold greater selectivity of c-Met targets versus FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB. Phase 1/2. | 
                                                        Mol Carcinog, 2021, 60(7):481-496 
                                                        G3 (Bethesda), 2021, 11(10)jkab265 
                                                        Mol Cell Biochem, 2018, 449(1-2):1-8 |   | 
                                
                                    
                                        | S7003 | AZD2932 | AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively. | 
                                                        Cancer Res, 2020, canres.1992.2020 
                                                        Molecules, 2020, 8;25(9) pii: E2220 
                                                        Development, 2016, 143(23):4394-4404 |  | 
                                
                                    
                                        | S0504 | SU14813 | SU14813 (SU 014813) is a multiple receptor tyrosine kinase inhibitor with IC50 of 50 nM, 2 nM, 4 nM and 15 nM for VEGFR2, VEGFR1, PDGFRβ and Kit (c-Kit). SU14813 exhibits potent antiangiogenic and antitumor activity. | 
                                                        Cancer Cell, 2022, S1535-6108(22)00312-9 
                                                        Adv Sci (Weinh), 2021, e2101848 |  | 
                                
                                    
                                        | S8721 | PDGFR inhibitor 1 | PDGFR inhibitor 1 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of Kit (c-Kit) and PDGFR with potential antineoplastic activity. It also inhibits several other kinases, including VEGFR2, TIE2, PDGFR-beta and CSF1R, thereby further inhibiting tumor cell growth. | 
                                                        bioRxiv, 2025, 2025.06.11.659120 
                                                        Elife, 2023, 12e79840 
                                                        Elife, 2023, 12e79840 |  | 
                                
                                    
                                        | S6526 | SKLB 610 | SKLB-610 is a multi-target inhibitor of the tyrosine kinases. It is most potent against VEGFR2 and exhibits slightly weaker inhibitor of FGFR2 and PDGFR. | 
                                                        Biomed Pharmacother, 2022, 149:112922 
                                                        Int J Mol Sci, 2022, 23(14)7853 |  | 
                                
                                    
                                        | S8161 | ON123300 | ON123300 is a potent and multi-targeted kinase inhibitor with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM for CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), and Fyn, respectively. | 
                                                        Cell Rep Med, 2025, S2666-3791(25)00231-9 
                                                        Cell Rep, 2024, 43(7):114446 
                                                        J Cell Sci, 2021, jcs.258685 |  | 
                                
                                    
                                        | S2895 | Tyrphostin 9 | Tyrphostin 9 (SF 6847, RG-50872) is firstly designed as an EGFR inhibitor with IC50 of 460 μM, but is also found to be more potent to PDGFR with IC50 of 0.5 μM. | 
                                                        Cell Rep, 2022, 38(10):110475 |  | 
                                
                                    
                                        | E4449 | AG 825 | AG-825 (Tyrphostin AG-825) is a potent and selective inhibitor of ErbB2 with IC50 values of 0.15 µM. It also inhibits  PDGFR autophosphorylation with IC50 value of 40 µM. It exhibits anti-cancer activity and significantly induces apoptosis in cancer cells. |  |  | 
                                
                                    
                                        | S7688 | Ki20227 | Ki20227 is an orally active and highly selective inhibitor of c-Fms tyrosine kinase(CSF1R) with IC50 of 2 nM, 12 nM, 451 nM and 217 nM for c-Fms, vascular endothelial growth factor receptor-2 (KDR/VEGFR-2), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor beta (PDGFRβ), respectively. | 
                                                        Cancer Immunol Immunother, 2024, 73(5):76 
                                                        Cancer Immunol Immunother, 2024, 73(5):76 |  | 
                                
                                    
                                        | S5272 | Toceranib phosphate | Toceranib phosphate (Palladia, SU11654), the phosphate salt of toceranib, is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR, and Kit with Ki values of 6 nM and 5 nM for Flk-1/KDR and PDGFRβ, respectively. | 
                                                        Front Vet Sci, 2024, 11:1392728 |  | 
                                
                                    
                                        | S4018 | Sennoside B | Sennoside B, a kind of irritant laxative isolated from rhei rhizome, inhibits PDGF-stimulated cell proliferation. |  |  | 
                                
                                    
                                        | S0763 | Tyrphostin AG1433 | Tyrphostin AG1433 (AG1433, SU1433) is a selective platelet-derived growth factor receptor β (PDGFRβ) and vascular endothelial growth factor receptor 2 (VEGFR-2, Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively. |  |  | 
                                
                                    
                                        | E0616 | Chiauranib | Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy. |  |  | 
                                
                                    
                                        | E2828New | AG 1295 | AG 1295 is a selective and specific inhibitor of platelet-derived growth factor receptor (PDGFR) tyrosine-kinase. It inhibits PDGFR autophosphorylation with IC50 values of 0.3-0.5 μM in membrane autophosphorylation assays, respectively. |  |  | 
                                
                                    
                                        | S6843 | Vorolanib | Vorolanib (X-82,CM082) is an oral, multikinase, dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with antiangiogenic and antineoplastic activities. |  |  | 
                                
                                    
                                        | E0814 | Masitinib mesylate | Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit with IC50 of 200 nM for human recombinant c-Kit, also inhibits PDGFRα/β with IC50s of 540/800 nM, Lyn with IC50 of 510 nM for LynB, and, to a lesser extent, FGFR3 and FAK. |  |  | 
                                
                                    
                                        | S8780 | AZD3229 | AZD3229 is a potent, pan-Kit (c-Kit) mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant Kit (c-Kit) driven Ba/F3 cell lines (GI50=1-50 nM), with good margin to KDR-driven effects. It also inhibits PDGFR mutants (Tel-PDGFRα, Tel-PDGFRβ, V561D/D842V). |  |  | 
                                
                                    
                                        | E2548 | N-(p-Coumaroyl) Serotonin | N-(p-Coumaroyl) Serotonin (p-coumaroylserotonin) is a polyphenol isolated from the seeds of safflower and has antioxidative, anti-atherogenic and anti-inflammatory properties, can inhibits PDGF-induced on phosphorylation of PDGF receptor and Ca2+ release from sarcoplasmic reticulum. |  |  | 
                                
                                    
                                        | E0050 | Seralutinib (GB002) | Seralutinib (PK10571, GB002) is a novel PDGFR kinase inhibitor with IC50s of 8 nM and 10 nM for PDGFRα and PDGFRβ in enzyme assays, respectively. |  |  | 
                                
                                    
                                        | E2393 | JNJ-10198409 | JNJ-10198409, a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor with IC50 of 2 nM, is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent, has good activity against PDGFRβ kinase and PDGFRα kinase with IC50 of 4.2 and 45 nM, respectively. |  |  | 
                                
                                    
                                        | S9973 | Flumatinib (HH-GV-678) | Flumatinib (HH-GV-678) is a novel inhibitor of Bcr-Abl with IC50 values of 1.2  nM, 307.6  nM and 665.5  nM for c-Abl, PDGFRβand c-Kit, respectively. |  |  |