VEGFR inhibitors/antagonists

Vascular Endothelial Growth Factor Receptor (VEGFR) is the receptor of VEGF. VEGFR is involved in cell proliferation, migration, survival and permeability. The VEGFs include five known structurally-related mammalian ligands (VEGFA, VEGFB, VEGFC, VEGFD, and placenta growth factor, PLGF) and there are also three structurally related VEGFRs subtypes (VEGFR1, VEGFR2, and VEGFR3). [show the full text]

Protein Tyrosine Kinase

EGFR IGF-1R c-Met c-Kit ALK Tie-2 HER2 PDGFR c-RET Trk receptor TAM receptors (Tyro-3,Axl,and Mertk) CSF-1R Ephrin receptor ACK DDR ROS1 Pyk2 Tyro3 Axl Mertk Fer kinase RON Insulin Receptor

Isoform-selective Products

VEGFR1 VEGFR2 VEGFR3

All (107)
VEGFR Inhibitors (105)
New VEGFR Products

Cat.No.	Product Name	Information	Product Use Citations
S1178	Regorafenib (BAY 73-4506)	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 (AG-013736)	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
S1119	Cabozantinib (XL184)	A potent VEGFR2 inhibitor with IC50 of 0.035 nM, Cabozantinib (XL184) also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. It induces PUMA-dependent apoptosis in colon cancer cells via AKT/GSK-3β/NF-κB signaling pathway.	Nat Commun, 2025, 16(1):509 Cell Death Differ, 2025, 10.1038/s41418-025-01510-x Cell Death Dis, 2025, 16(1):76
S1010	Nintedanib (BIBF 1120)	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
S1046	Vandetanib	Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. This compound increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).	Virulence, 2025, 16(1):2489751 bioRxiv, 2025, 2024.12.19.629395 bioRxiv, 2025, 2024.12.19.629395
S1164	Lenvatinib (E7080)	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. This compound 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 Cancer, 2025, 10.1038/s43018-025-01058-2
S4001	Cabozantinib malate	Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. This compound induces apoptosis.	Sci Rep, 2025, 15(1):35889 bioRxiv, 2025, 2025.08.15.670608 Nat Neurosci, 2024, 10.1038/s41593-024-01604-8
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. This compound induces cathepsin B activation and autophagy.	Nucleic Acids Res, 2025, 53(4)gkaf107 Commun Biol, 2025, 8(1):1185 Sci Rep, 2025, 15(1):35889
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, and shows similar activity against c-Kit and PDGFRβ. It is 36-, 110-fold and >1000-fold more selective for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. This compound induces autophagic vacuole accumulation and is in 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
S1101	Vatalanib (PTK787) 2HCl	Vatalanib 2HCl (PTK787, ZK 222584, cpg-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM in a cell-free assay, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 3.	Nat Commun, 2025, 16(1):7287 Environ Health Perspect, 2024, 132(5):57001 J Cancer, 2024, 15(9):2448-2459
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
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
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). This compound induces autophagy and apoptosis, and is in Phase 3.	Biomed Pharmacother, 2024, 180:117533 Cell Death Discov, 2023, 9(1):57 Cell Death Discov, 2023, 9(1):57
S8726	Anlotinib (AL3818) dihydrochloride	Anlotinib (AL3818) is a highly potent and selective VEGFR2 inhibitor with IC50 less than 1 nM. It has broad-spectrum antitumor potential in clinical trials. Please use saline solution rather than PBS for dilutions. PBS may cause precipitation.	J Immunother Cancer, 2025, 13(9)e010812 Clin Transl Med, 2025, 15(2):e70228 Commun Biol, 2025, 8(1):1185
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)). This compound has potential antineoplastic activity.	Nat Commun, 2024, 15(1):1754 iScience, 2024, 27(10):110862 J Hepatocell Carcinoma, 2023, 10:697-712
S2842	SAR131675	SAR131675 is a VEGFR3 inhibitor with IC50/K_i of 23 nM/12 nM in cell-free assays, about 50- and 10-fold more selective for VEGFR3 than VEGFR1/2, little activity against Akt1, CDKs, PLK1, EGFR, IGF-1R, c-Met, Flt2 etc.	Cell Death Discov, 2025, 11(1):320 Zool Res, 2025, 46(6):1317-1325 Cell Signal, 2025, 130:111675
S5248	Apatinib	Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib induces both autophagy and apoptosis.	Ann Dermatol, 2025, 37(4):228-240 Discov Oncol, 2025, 16(1):930 Cancer Cell, 2024, 42(4):535-551.e8
S2221	Apatinib (YN968D1) mesylate	Apatinib mesylate (YN968D1, Rivoceranib) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib mesylate induces both autophagy and apoptosis.	Oncol Res, 2025, 33(6):1459-1472 Clin Respir J, 2024, 18(2):e13738 Clin Respir J, 2024, 18(2):e13738
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
S2896	ZM 323881 HCl	ZM 323881 is a potent and selective VEGFR2 inhibitor with IC50 of <2 nM, almost no activity on VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2.	Cell Commun Signal, 2025, 23(1):113 Invest Ophthalmol Vis Sci, 2025, 66(12):45 Stem Cells Transl Med, 2023, szad049
S2845	Semaxanib (SU5416)	Semaxanib (SU5416, semaxinib) is a potent and selective VEGFR(Flk-1/KDR) inhibitor with IC50 of 1.23 μM, 20-fold more selective for VEGFR than PDGFRβ, and lacks activity against EGFR, InsR and FGFR. Phase 3. It can be used to induce animal models of chronic intermittent hypoxia.	Clin Sci (Lond), 2025, 139(10)CS20255922 bioRxiv, 2025, 2025.01.24.634732 Nat Commun, 2024, 15(1):4758
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
S5242	Cediranib Maleate	Cediranib Maleate (AZD2171) is the maleate salt of Cediranib, which is a potent inhibitor of VEGFR with IC50 of <1 nM and also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM.	J Exp Clin Cancer Res, 2024, 43(1):56 Cell Oncol (Dordr), 2022, 45(4):601-619 Mol Cancer Ther, 2022, 21(6):1030-1043
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. It shows similar activity against Kit (c-Kit) and is ~10-fold more selective for VEGFR than PDGFR and Ret. This compound is in 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
S1084	Brivanib (BMS-540215)	Brivanib (BMS-540215) is an ATP-competitive inhibitor with an IC50 of 25 nM against VEGFR2, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. It is in Phase 3.	Biomed Pharmacother, 2024, 180:117533 Stem Cells Transl Med, 2023, szad049 Stem Cells Transl Med, 2023, 12(10):676-688
S2897	ZM 306416	ZM 306416 (CB 676475) is a VEGFR (Flt and KDR) inhibitor for VEGFR1 with IC50 of 0.33 μM, but also found to inhibit EGFR with IC50 of <10 nM.	Nat Commun, 2024, 15(1):4758 Int J Mol Sci, 2024, 25(5)2956 J Pharmacol Sci, 2023, 151(4):177-186
S5793	Motesanib (AMG-706)	Motesanib (AMG-706) is an orally bioavailable receptor tyrosine kinase inhibitor with IC50 values of 2 nM, 3 nM, 6 nM, 8 nM, 84 nM, 59 nM for VEGFR1, VEGFR2, VEGFR3, Kit, PDGFR and Ret, respectively.	Signal Transduct Target Ther, 2022, 7(1):147 Front Cell Dev Biol, 2022, 10:836179 J Pharm Sci, 2022, 111(8):2180-2190
S1557	KRN 633	KRN 633 is an ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 170 nM/160 nM/125 nM, weakly inhibits PDGFR-α/β and c-Kit, does not block the phosphorylation of FGFR-1, EGFR or c-Met in cell.	Aust Dent J, 2020, 10.1111/adj.12752 J Med Invest, 2017, 64(3.4):262-265 Oncotarget, 2016, 7(5):5985-99
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
S5667	Fruquintinib (HMPL-013)	Fruquintinib is a small molecule inhibitor with strong potency and high selectivity against VEGFR family. It inhibits VEGFR 1, 2, 3, with IC50 values of 33 nM, 35 nM and 0.5 nM, respectively and shows only weak inhibition of RET, FGFR-1 and c-kit kinases.	Sci Adv, 2025, 11(20):eads1631 EMBO J, 2024, 43(8):1519-1544 iScience, 2024, 27(10):110862
S7258	SKLB1002	SKLB1002 is a potent and ATP-competitive VEGFR2 inhibitor with IC50 of 32 nM.	Sci Rep, 2025, 15(1):8177 Sci Adv, 2024, 10(20):eadl0633 Sci Adv, 2024, 10(20):eadl0633
S2366	Taxifolin (Dihydroquercetin)	Taxifolin (Dihydroquercetin), a flavonoid in many plants such as Taxus chinensis, Siberian larch, Cedrus deodara and so on, is a type I inhibitor for VEGFR-2 kinase.	J Virol, 2025, e0209524. Sci Rep, 2020, 10(1):17311 J Med Virol, 2019, 91(8):1440-1447
S1138	Brivanib Alaninate (BMS-582664)	Brivanib alaninate (BMS-582664) is the prodrug of BMS-540215, an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM.	Int J Oncol, 2014, 44(3):959-69 Assay Drug Dev Technol, 2014, 12(9-10):514-26
S8189	BAW2881 (NVP-BAW2881)	BAW2881 (NVP-BAW2881) is a novel vascular endothelial growth factor (VEGF) receptor tyrosine-kinase inhibitor that potently inhibits VEGFR1-3 at 1.0-4.3 nanomolar (nM) concentrations and inhibits PDGFRβ, c-Kit, and RET (c-RET) at 45-72 nM concentrations.	J Transl Med, 2025, 23(1):985 JCI Insight, 2021, 143285 J Cell Biochem, 2019, 120(4):5583-5596
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). This compound exhibits potent antiangiogenic and antitumor activity.	Cancer Cell, 2022, S1535-6108(22)00312-9 Adv Sci (Weinh), 2021, e2101848
S6535	SU1498	SU1498, a powerful inhibitor of KDR (IC50 = 0.7 μM), stimulates accumulation of phosphorylated ERK1/2 in endothelial cells.	Cell Metab, 2020, 5;31(5):892-908 e11 Biol Open, 2018,
S0278	SU5614	SU5614 (Chloro-SU5416, Chloro-Semaxanib) is a small molecule receptor tyrosine kinases (RTK) inhibitor of VEGFR-2, c-kit, and both wild-type and mutant FLT3. This compound reduces cell proliferation and induces apoptosis.	Am J Pathol, 2024, S0002-9440(24)00326-2 Adv Sci (Weinh), 2021, e2101848 Front Cell Dev Biol, 2021, 9:797047
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
S6514	SU5408	SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and selective inhibitor of VEGFR2 Kinase with IC50 of 70 nM.	Transl Oncol, 2022, 25:101516 J Dent Sci, 2022, 17(4):1471-1479
S0290	SU5204	SU5204 is a tyrosine kinase inhibitor with IC50 of 4 μM and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively.	Front Pharmacol, 2021, 12:804327
S6520	WHI-P180	WHI-P180 is a multi-kinase inhibitor with IC50 values of 4.5 and 66 nM for the human proto-oncogene RET (c-RET) and kinase insert domain receptor (KDR), respectively.
S6543	ZD-4190	ZD-4190 is a submicromolar inhibitor of VEGF RTK activity in vitro with IC50 values of 29 ± 4 nM and 708 ± 63 nM for KDR and Flt-1, respectively.
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
S8188	BFH772	BFH772 is a novel potent oral VEGFR2 inhibitor, targeting VEGFR2 kinase with IC50 of 3 nM.
S0291	SU5208	SU5208(3-[(Thien-2-yl)methylene]-2-indolinone) is an inhibitor of vascular endothelial growth factor receptor-2 (VEGFR2).
E2397	hVEGF-IN-1	hVEGF-IN-1, a quinazoline derivative, specifically binds to the G-rich sequence in the internal ribosome entry site A (IRES-A) with a Kd of 0.928 μM, therefore destabilizes the G-quadruplex structure, , also hinders tumor cells migration and represses tumor growth by decreasing VEGF-A protein expression.
S0765	MAZ51	MAZ51 is a potent and selective inhibitor of vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase. This compound induces cell rounding and G2/M cell cycle arrest in glioma cells through phosphorylation of Akt/GSK3β and activation of RhoA. It inhibits the proliferation and induces the apoptosis of a variety of non-VEGFR-3-expressing tumor cell lines.	Sci Rep, 2025, 15(1):1283
E2656	R1530	R1530 is a highly potent, orally bioavailable, dual-acting mitosis/angiogenesis inhibitor for the treatment of solid tumors, which can inhibit vascular endothelial growth factor receptor 2 (VEGFR2) and fibroblast growth factor receptors 1 (FGFR1) with IC50s of 10 nM and 28 nM, respectively.
E1078	Emvododstat (PTC299)	Emvododstat (PTC299) is a post-transcriptional inhibitor of pathogenic VEGF and dihydroorotate dehydrogenase(DHODH), which inhibits VEGFA mRNA translation and abnormal cell proliferation. In HeLa cells, this compound inhibits hypoxia-induced VEGFA protein production with an EC50 of 1.64 nM.
S2211	AG-13958	AG-13958 (AG-013958), a VEGFR tyrosine kinase inhibitor, is in clinical development with ST administration for treatment of choroidal neovascularization associated with age–related macular degeneration (AMD).
S5607	4,4'-Bis(4-aminophenoxy)biphenyl	4,4'-Bis(4-aminophenoxy)biphenyl is a monomer for polyimide production.
S7647	Lucitanib (E3810) hydrochloride	Lucitanib (E-3810, AL3810) hydrochloride is a dual inhibitor of Vascular endothelial growth factor receptor (VEGFR) and Fibroblast growth factor receptor (FGFR). Lucitanib hydrochloride (E-3810, AL3810) potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50 of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.	Sci Rep, 2023, 13(1):20223
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.
S6764	Pamufetinib (TAS-115)	Pamufetinib (TAS-115) is a highly potent c-Met and VEGFR dual inhibitor with IC50s of 30 nM and 32 nM for recombinant VEGFR2 and recombinant MET, respectively.
E3379	Cassia seed Extract	Cassia seed Extract is extracted from seed of Cassia toraLinn, has the potential to influence varieties of biological processes and pathways, including positive regulation of smooth muscle cell proliferation, inflammatory response, tumor necrosis factor (TNF) signaling pathway, vascular endothelial growth factor (VEGF) signaling pathway and arachidonic acid (ARA) metabolism.
S0377	CS-2660 (JNJ-38158471)	CS-2660 (JNJ-38158471) is a well tolerated, orally available, highly selective VEGFR-2 inhibitor with IC50 of 40 nM. This compound also inhibits closely related tyrosine kinases such as RET (c-RET) and Kit (c-Kit) with IC50 of 180 nM and 500 nM，while it has no significant activity (>1 microM) against VEGFR-1 and VEGFR-3.
E0534	WAY-340935	WAY-340935 (VEGFR2-IN-2) can inhibit the function of VEGFR2 and the anti-proliferative activity against the H460 cell line is produced partly by interaction of VEGFR protein.
S9402	(20R)-Protopanaxadiol	(20R)-Protopanaxadiol, isolated from the roots of Panax ginseng, has protective effect on myocardial ischemia.
E3414	Semen litchi Extract	Semen litchi Extract is extracted from Litchi chinensis, which has an anti-hepatoma effect and inhibits angiogenesis by targeting VEGFR in hepatocellular carcinoma.
E3774	Chlorella Pyrenoidosa Extract	Chlorella Pyrenoidosa Extract is extracted from Chlorella pyrenoidosa, which exerts a significant antiangiogenic activity was observed against VEGF-induced neovascularization and antiproliferative activity.
E4694	EVT801	EVT801 is a potent and selective inhibitor of VEGFR-3 with an IC50 of 11 nM. It exhibits potent antitumor effects and represents a promising anti-lymphangiogenic drug in patients with VEGFR-3 positive tumors.
S6808	SU5205	SU5205 is an inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 9.6 µM.
S7397	Sorafenib (BAY 43-9006)	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
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. This compound 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. It 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
S7781	Sunitinib (SU-11248)	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 J Exp Clin Cancer Res, 2025, 44(1):290
S1490	Ponatinib (AP24534)	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 J Exp Clin Cancer Res, 2025, 44(1):290
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.	Nat Commun, 2025, 16(1):7853 CNS Neurosci Ther, 2025, 31(12):e70696 Sci Rep, 2025, 15(1):35889
S1029	Lenalidomide (CC-5013)	Lenalidomide is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.	Signal Transduct Target Ther, 2025, 10(1):29 Nat Commun, 2025, 16(1):3800 Cell Rep Med, 2025, S2666-3791(25)00102-8
S1264	PD173074	PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells.	Stem Cell Reports, 2025, 20(10):102640 Commun Biol, 2025, 8(1):125 Cell Stem Cell, 2024, S1934-5909(24)00294-7
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
S1018	Dovitinib (TKI-258)	Dovitinib (TKI-258, CHIR258) is a multitargeted RTK inhibitor, primarily targeting class III RTKs (FLT3/c-Kit) with IC50 values of 1 nM/2 nM. It is also potent against class IV (FGFR1/3) and class V (VEGFR1-4) RTKs, exhibiting IC50 values of 8–13 nM, while showing lower potency toward 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
S8064	Midostaurin (PKC412)	Midostaurin is a multi-targeted kinase inhibitor, including PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50 ranging from 80-500 nM.	Blood Adv, 2025, bloodadvances.2024015427 Onco Targets Ther, 2025, 18:489-501 Blood Cancer J, 2024, 14(1):207
S8401	Erdafitinib (JNJ-42756493)	Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. This compound 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
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
S2161	RAF265 (CHIR-265)	RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM in cell-free assays. This compound induces cell cycle arrest and apoptosis. Phase 2.	bioRxiv, 2025, 2025.04.29.651188 Cancer Cell, 2022, S1535-6108(22)00312-9 iScience, 2022, 25(10):105182
S7057	LY2874455	LY2874455 is a pan-FGFR inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM. Phase 1.	Cancer Drug Resist, 2025, 8:45 Cancer Discov, 2023, 13(9):1998-2011 Cancer Discov, 2023, 13(9):1998-2011
S1486	AEE788 (NVP-AEE788)	AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, respectively. It is less potent against VEGFR2/KDR, c-Abl, c-Src, and Flt-1, and does not inhibit Ins-R, IGF-1R, PKCα, or CDK1. This compound has reached Phase 1/2 clinical trials.	Cell Rep Med, 2022, 3(1):100492 Genome Med, 2020, 18;12(1):17 Oncotarget, 2019, 10(68):7185-7197
S1361	MGCD-265 analog	MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2.	Cancer Cell, 2022, S1535-6108(22)00312-9 Cell Rep Med, 2022, 3(1):100492 Protein Cell, 2019, 10(3):161-177
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. This compound 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
S1171	CYC116	CYC116 is a potent inhibitor of Aurora A/B with K_i of 8.0 nM/9.2 nM, is less potent to VEGFR2 (K_i of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1.	Sci Rep, 2024, 14(1):4303 Cell Chem Biol, 2023, 30(8):987-998.e24 Proc Natl Acad Sci U S A, 2022, 119(15):e2122512119
S2859	Golvatinib (E7050)	Golvatinib (E7050) is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, respectively. This compound does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM) and is currently in Phase 1/2 trials.	Int J Mol Sci, 2023, 24(11)9606 Int J Mol Sci, 2022, 23(23)14884 Cancer Sci, 2020, 111(10):3813-3823
S1220	OSI-930	OSI-930 is a potent inhibitor of Kit (c-Kit), KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; this compound is also potent to Flt-1, c-Raf and Lck and has low activity against PDGFRα/β, Flt-3 and Abl. Phase 1.	Nat Commun, 2024, 15(1):4739 Cell Rep, 2019, 28(9):2331-2344 Nat Biomed Eng, 2018, 2(8):578-588
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
S8573	Sitravatinib (MGCD516)	Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.	Commun Biol, 2025, 8(1):1185 Res Sq, 2025, rs.3.rs-6431257 JCI Insight, 2022, e148717
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
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.	Res Sq, 2025, rs.3.rs-7032881 bioRxiv, 2025, 2025.06.11.659120 Elife, 2023, 12e79840
S6412	Altiratinib	Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor of TRK, Met (c-Met), TIE2, and VEGFR2 kinases with IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. This compound inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM.	J Microbiol, 2025, 63(2):e2409001 Theranostics, 2021, 11(20):9918-9936 Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
S2201	BMS-794833	BMS-794833 is a potent ATP competitive inhibitor of Met (c-Met)/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378. Phase 1.	Cell Stem Cell, 2025, 32(11):1671-1690.e13 Cancer Res, 2021, canres.1428.2021
S0487	Sulfatinib	Sulfatinib is a potent and highly selective tyrosine kinase inhibitor against VEGFR1, VEGFR2, VEGFR3, FGFR1 and CSF1R with IC50 of 2 nM, 24 nM, 1 nM, 15 nM and 4 nM, respectively. This compound shows encouraging antitumor activity and manageable toxicities in patients with advanced NETs.	Front Oncol, 2023, 13:1158857
S2018	ENMD-2076 L-(+)-Tartaric acid	ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more selective for Aurora A than Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.
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
S8882	ODM-203	ODM-203 is a selective inhibitor of FGFR and VEGFR with ic50s of 11 nM,16 nM,6 nM, 35 nM,26 nM,9 nM,5 nM for recombinant FGFR1, FGFR2, FGFR3,FGFR4, VEGFR1, VEGFR2 and VEGFR3, respectively.
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.
E0499	4SC-203	4SC-203 (SC71710) is a multikinase inhibitor with potential antineoplastic activity. This compound selectively inhibits FMS-related tyrosine kinase 3 (FLT3/STK1), FLT3 mutated forms, and vascular endothelial growth factor receptors (VEGFRs).
S9621	Donafenib (Sorafenib D3)	Donafenib (Sorafenib D3, Bay 43-9006 D3, CM-4307) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 15 nM, 20 nM and 22 nM for Raf-1, mVEGFR-2, mVEGFR-3 and B-RAF, 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.
S6870	Ningetinib	Ningetinib (CT-053, DE-120, CT053PTSA) is a potent, orally bioavailable inhibitor of tyrosine kinase with IC50 of 6.7 nM, 1.9 nM and <1.0 nM for c-Met, VEGFR2 and Axl, respectively. This compound exhibits antitumor activity.
S6939	Nastorazepide	Nastorazepide (Z-360), a cholecystokinin-2/gastrin receptor (CCK2/gastrin receptor) antagonist, combines with gemcitabine prolonged survival and reduces gemcitabine-induced vascular endothelial growth factor (VEGF) expression in a pancreatic carcinoma orthotopic xenograft mouse.
E4914	Cabozantinib hydrochloride	Cabozantinib hydrochloride(XL184, BMS-907351 hydrochloride) is a potent small-molecule kinase inhibitor of c-MET and VEGFR2 with an IC50 of 1.3 nM, 0.035 nM respectively. It also inhibits RET, KIT, AXL, Tie2 and FLT3 with an IC50's of 5.2 nM, 4.6 nM, 7 nM, 14.3 nM, 11.3nM respectively. It can be promising agent for inhibiting tumor angiogenesis and metastasis in cancers with dysregulated MET and VEGFR signaling.
S4686	Vitamin E	Vitamin E (D-alpha-Tocopherol) is a fat-soluble vitamin with potent antioxidant properties. It is a potent peroxyl radical scavenger and inhibits noncompetitively cyclooxygenase activity in many tissues, also inhibits angiogenesis and tumor dormancy through suppressing vascular endothelial growth factor (VEGF) gene transcription.	Elife, 2025, 13RP94169 Cancer Drug Resist, 2025, 8:45 Signal Transduct Target Ther, 2024, 9(1):109
E0207	Chebulinic acid	Chebulinic acid, a phenolic compound isolated from Terminalia chebula fruit, is a novel Influenza viral neuraminidase inhibitor. This compound is a antiangiogenic agent through inhibiting the actions of VEGF. It shows antitumour activity.
S6809	SU5214	SU5214 is a inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 14.8 µM and EGFR with IC50 of 36.7 µm, respectively.
E1435	Tinengotinib	Tinengotinib (TT-00420) is a novel multiple kinase inhibitor that strongly inhibits Aurora A/B with IC50 values of 1.2/3.3 nM respectively. It also exhibits potent inhibitory activity on FGFR1/2/3, VEGFR1, JAK1/2, and CSF1R and can be used to treat several prominent signaling pathways in triple-negative breast cancer(TNBC).
E0142	XL092	XL092 (JUN04542) is an ATP-competitive inhibitor of multiple RTKs including MET, VEGFR2, AXL and MER, with IC50 values of 15 nM, 1.6 nM, 3.4 nM, and 7.2 nM in cell-based assays, respectively.
S1178	Regorafenib (BAY 73-4506)	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 (AG-013736)	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
S1119	Cabozantinib (XL184)	A potent VEGFR2 inhibitor with IC50 of 0.035 nM, Cabozantinib (XL184) also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. It induces PUMA-dependent apoptosis in colon cancer cells via AKT/GSK-3β/NF-κB signaling pathway.	Nat Commun, 2025, 16(1):509 Cell Death Differ, 2025, 10.1038/s41418-025-01510-x Cell Death Dis, 2025, 16(1):76
S1010	Nintedanib (BIBF 1120)	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
S1046	Vandetanib	Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. This compound increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).	Virulence, 2025, 16(1):2489751 bioRxiv, 2025, 2024.12.19.629395 bioRxiv, 2025, 2024.12.19.629395
S1164	Lenvatinib (E7080)	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. This compound 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 Cancer, 2025, 10.1038/s43018-025-01058-2
S4001	Cabozantinib malate	Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. This compound induces apoptosis.	Sci Rep, 2025, 15(1):35889 bioRxiv, 2025, 2025.08.15.670608 Nat Neurosci, 2024, 10.1038/s41593-024-01604-8
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. This compound induces cathepsin B activation and autophagy.	Nucleic Acids Res, 2025, 53(4)gkaf107 Commun Biol, 2025, 8(1):1185 Sci Rep, 2025, 15(1):35889
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, and shows similar activity against c-Kit and PDGFRβ. It is 36-, 110-fold and >1000-fold more selective for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. This compound induces autophagic vacuole accumulation and is in 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
S1101	Vatalanib (PTK787) 2HCl	Vatalanib 2HCl (PTK787, ZK 222584, cpg-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM in a cell-free assay, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 3.	Nat Commun, 2025, 16(1):7287 Environ Health Perspect, 2024, 132(5):57001 J Cancer, 2024, 15(9):2448-2459
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
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
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). This compound induces autophagy and apoptosis, and is in Phase 3.	Biomed Pharmacother, 2024, 180:117533 Cell Death Discov, 2023, 9(1):57 Cell Death Discov, 2023, 9(1):57
S8726	Anlotinib (AL3818) dihydrochloride	Anlotinib (AL3818) is a highly potent and selective VEGFR2 inhibitor with IC50 less than 1 nM. It has broad-spectrum antitumor potential in clinical trials. Please use saline solution rather than PBS for dilutions. PBS may cause precipitation.	J Immunother Cancer, 2025, 13(9)e010812 Clin Transl Med, 2025, 15(2):e70228 Commun Biol, 2025, 8(1):1185
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)). This compound has potential antineoplastic activity.	Nat Commun, 2024, 15(1):1754 iScience, 2024, 27(10):110862 J Hepatocell Carcinoma, 2023, 10:697-712
S2842	SAR131675	SAR131675 is a VEGFR3 inhibitor with IC50/K_i of 23 nM/12 nM in cell-free assays, about 50- and 10-fold more selective for VEGFR3 than VEGFR1/2, little activity against Akt1, CDKs, PLK1, EGFR, IGF-1R, c-Met, Flt2 etc.	Cell Death Discov, 2025, 11(1):320 Zool Res, 2025, 46(6):1317-1325 Cell Signal, 2025, 130:111675
S5248	Apatinib	Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib induces both autophagy and apoptosis.	Ann Dermatol, 2025, 37(4):228-240 Discov Oncol, 2025, 16(1):930 Cancer Cell, 2024, 42(4):535-551.e8
S2221	Apatinib (YN968D1) mesylate	Apatinib mesylate (YN968D1, Rivoceranib) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib mesylate induces both autophagy and apoptosis.	Oncol Res, 2025, 33(6):1459-1472 Clin Respir J, 2024, 18(2):e13738 Clin Respir J, 2024, 18(2):e13738
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
S2896	ZM 323881 HCl	ZM 323881 is a potent and selective VEGFR2 inhibitor with IC50 of <2 nM, almost no activity on VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2.	Cell Commun Signal, 2025, 23(1):113 Invest Ophthalmol Vis Sci, 2025, 66(12):45 Stem Cells Transl Med, 2023, szad049
S2845	Semaxanib (SU5416)	Semaxanib (SU5416, semaxinib) is a potent and selective VEGFR(Flk-1/KDR) inhibitor with IC50 of 1.23 μM, 20-fold more selective for VEGFR than PDGFRβ, and lacks activity against EGFR, InsR and FGFR. Phase 3. It can be used to induce animal models of chronic intermittent hypoxia.	Clin Sci (Lond), 2025, 139(10)CS20255922 bioRxiv, 2025, 2025.01.24.634732 Nat Commun, 2024, 15(1):4758
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
S5242	Cediranib Maleate	Cediranib Maleate (AZD2171) is the maleate salt of Cediranib, which is a potent inhibitor of VEGFR with IC50 of <1 nM and also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM.	J Exp Clin Cancer Res, 2024, 43(1):56 Cell Oncol (Dordr), 2022, 45(4):601-619 Mol Cancer Ther, 2022, 21(6):1030-1043
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. It shows similar activity against Kit (c-Kit) and is ~10-fold more selective for VEGFR than PDGFR and Ret. This compound is in 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
S1084	Brivanib (BMS-540215)	Brivanib (BMS-540215) is an ATP-competitive inhibitor with an IC50 of 25 nM against VEGFR2, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. It is in Phase 3.	Biomed Pharmacother, 2024, 180:117533 Stem Cells Transl Med, 2023, szad049 Stem Cells Transl Med, 2023, 12(10):676-688
S2897	ZM 306416	ZM 306416 (CB 676475) is a VEGFR (Flt and KDR) inhibitor for VEGFR1 with IC50 of 0.33 μM, but also found to inhibit EGFR with IC50 of <10 nM.	Nat Commun, 2024, 15(1):4758 Int J Mol Sci, 2024, 25(5)2956 J Pharmacol Sci, 2023, 151(4):177-186
S5793	Motesanib (AMG-706)	Motesanib (AMG-706) is an orally bioavailable receptor tyrosine kinase inhibitor with IC50 values of 2 nM, 3 nM, 6 nM, 8 nM, 84 nM, 59 nM for VEGFR1, VEGFR2, VEGFR3, Kit, PDGFR and Ret, respectively.	Signal Transduct Target Ther, 2022, 7(1):147 Front Cell Dev Biol, 2022, 10:836179 J Pharm Sci, 2022, 111(8):2180-2190
S1557	KRN 633	KRN 633 is an ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 170 nM/160 nM/125 nM, weakly inhibits PDGFR-α/β and c-Kit, does not block the phosphorylation of FGFR-1, EGFR or c-Met in cell.	Aust Dent J, 2020, 10.1111/adj.12752 J Med Invest, 2017, 64(3.4):262-265 Oncotarget, 2016, 7(5):5985-99
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
S5667	Fruquintinib (HMPL-013)	Fruquintinib is a small molecule inhibitor with strong potency and high selectivity against VEGFR family. It inhibits VEGFR 1, 2, 3, with IC50 values of 33 nM, 35 nM and 0.5 nM, respectively and shows only weak inhibition of RET, FGFR-1 and c-kit kinases.	Sci Adv, 2025, 11(20):eads1631 EMBO J, 2024, 43(8):1519-1544 iScience, 2024, 27(10):110862
S7258	SKLB1002	SKLB1002 is a potent and ATP-competitive VEGFR2 inhibitor with IC50 of 32 nM.	Sci Rep, 2025, 15(1):8177 Sci Adv, 2024, 10(20):eadl0633 Sci Adv, 2024, 10(20):eadl0633
S2366	Taxifolin (Dihydroquercetin)	Taxifolin (Dihydroquercetin), a flavonoid in many plants such as Taxus chinensis, Siberian larch, Cedrus deodara and so on, is a type I inhibitor for VEGFR-2 kinase.	J Virol, 2025, e0209524. Sci Rep, 2020, 10(1):17311 J Med Virol, 2019, 91(8):1440-1447
S1138	Brivanib Alaninate (BMS-582664)	Brivanib alaninate (BMS-582664) is the prodrug of BMS-540215, an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM.	Int J Oncol, 2014, 44(3):959-69 Assay Drug Dev Technol, 2014, 12(9-10):514-26
S8189	BAW2881 (NVP-BAW2881)	BAW2881 (NVP-BAW2881) is a novel vascular endothelial growth factor (VEGF) receptor tyrosine-kinase inhibitor that potently inhibits VEGFR1-3 at 1.0-4.3 nanomolar (nM) concentrations and inhibits PDGFRβ, c-Kit, and RET (c-RET) at 45-72 nM concentrations.	J Transl Med, 2025, 23(1):985 JCI Insight, 2021, 143285 J Cell Biochem, 2019, 120(4):5583-5596
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). This compound exhibits potent antiangiogenic and antitumor activity.	Cancer Cell, 2022, S1535-6108(22)00312-9 Adv Sci (Weinh), 2021, e2101848
S6535	SU1498	SU1498, a powerful inhibitor of KDR (IC50 = 0.7 μM), stimulates accumulation of phosphorylated ERK1/2 in endothelial cells.	Cell Metab, 2020, 5;31(5):892-908 e11 Biol Open, 2018,
S0278	SU5614	SU5614 (Chloro-SU5416, Chloro-Semaxanib) is a small molecule receptor tyrosine kinases (RTK) inhibitor of VEGFR-2, c-kit, and both wild-type and mutant FLT3. This compound reduces cell proliferation and induces apoptosis.	Am J Pathol, 2024, S0002-9440(24)00326-2 Adv Sci (Weinh), 2021, e2101848 Front Cell Dev Biol, 2021, 9:797047
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
S6514	SU5408	SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and selective inhibitor of VEGFR2 Kinase with IC50 of 70 nM.	Transl Oncol, 2022, 25:101516 J Dent Sci, 2022, 17(4):1471-1479
S0290	SU5204	SU5204 is a tyrosine kinase inhibitor with IC50 of 4 μM and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively.	Front Pharmacol, 2021, 12:804327
S6520	WHI-P180	WHI-P180 is a multi-kinase inhibitor with IC50 values of 4.5 and 66 nM for the human proto-oncogene RET (c-RET) and kinase insert domain receptor (KDR), respectively.
S6543	ZD-4190	ZD-4190 is a submicromolar inhibitor of VEGF RTK activity in vitro with IC50 values of 29 ± 4 nM and 708 ± 63 nM for KDR and Flt-1, respectively.
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
S8188	BFH772	BFH772 is a novel potent oral VEGFR2 inhibitor, targeting VEGFR2 kinase with IC50 of 3 nM.
S0291	SU5208	SU5208(3-[(Thien-2-yl)methylene]-2-indolinone) is an inhibitor of vascular endothelial growth factor receptor-2 (VEGFR2).
E2397	hVEGF-IN-1	hVEGF-IN-1, a quinazoline derivative, specifically binds to the G-rich sequence in the internal ribosome entry site A (IRES-A) with a Kd of 0.928 μM, therefore destabilizes the G-quadruplex structure, , also hinders tumor cells migration and represses tumor growth by decreasing VEGF-A protein expression.
S0765	MAZ51	MAZ51 is a potent and selective inhibitor of vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase. This compound induces cell rounding and G2/M cell cycle arrest in glioma cells through phosphorylation of Akt/GSK3β and activation of RhoA. It inhibits the proliferation and induces the apoptosis of a variety of non-VEGFR-3-expressing tumor cell lines.	Sci Rep, 2025, 15(1):1283
E2656	R1530	R1530 is a highly potent, orally bioavailable, dual-acting mitosis/angiogenesis inhibitor for the treatment of solid tumors, which can inhibit vascular endothelial growth factor receptor 2 (VEGFR2) and fibroblast growth factor receptors 1 (FGFR1) with IC50s of 10 nM and 28 nM, respectively.
E1078	Emvododstat (PTC299)	Emvododstat (PTC299) is a post-transcriptional inhibitor of pathogenic VEGF and dihydroorotate dehydrogenase(DHODH), which inhibits VEGFA mRNA translation and abnormal cell proliferation. In HeLa cells, this compound inhibits hypoxia-induced VEGFA protein production with an EC50 of 1.64 nM.
S2211	AG-13958	AG-13958 (AG-013958), a VEGFR tyrosine kinase inhibitor, is in clinical development with ST administration for treatment of choroidal neovascularization associated with age–related macular degeneration (AMD).
S5607	4,4'-Bis(4-aminophenoxy)biphenyl	4,4'-Bis(4-aminophenoxy)biphenyl is a monomer for polyimide production.
S7647	Lucitanib (E3810) hydrochloride	Lucitanib (E-3810, AL3810) hydrochloride is a dual inhibitor of Vascular endothelial growth factor receptor (VEGFR) and Fibroblast growth factor receptor (FGFR). Lucitanib hydrochloride (E-3810, AL3810) potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50 of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.	Sci Rep, 2023, 13(1):20223
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.
S6764	Pamufetinib (TAS-115)	Pamufetinib (TAS-115) is a highly potent c-Met and VEGFR dual inhibitor with IC50s of 30 nM and 32 nM for recombinant VEGFR2 and recombinant MET, respectively.
S0377	CS-2660 (JNJ-38158471)	CS-2660 (JNJ-38158471) is a well tolerated, orally available, highly selective VEGFR-2 inhibitor with IC50 of 40 nM. This compound also inhibits closely related tyrosine kinases such as RET (c-RET) and Kit (c-Kit) with IC50 of 180 nM and 500 nM，while it has no significant activity (>1 microM) against VEGFR-1 and VEGFR-3.
E0534	WAY-340935	WAY-340935 (VEGFR2-IN-2) can inhibit the function of VEGFR2 and the anti-proliferative activity against the H460 cell line is produced partly by interaction of VEGFR protein.
E3414	Semen litchi Extract	Semen litchi Extract is extracted from Litchi chinensis, which has an anti-hepatoma effect and inhibits angiogenesis by targeting VEGFR in hepatocellular carcinoma.
E3774	Chlorella Pyrenoidosa Extract	Chlorella Pyrenoidosa Extract is extracted from Chlorella pyrenoidosa, which exerts a significant antiangiogenic activity was observed against VEGF-induced neovascularization and antiproliferative activity.
E4694	EVT801	EVT801 is a potent and selective inhibitor of VEGFR-3 with an IC50 of 11 nM. It exhibits potent antitumor effects and represents a promising anti-lymphangiogenic drug in patients with VEGFR-3 positive tumors.
S6808	SU5205	SU5205 is an inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 9.6 µM.
S7397	Sorafenib (BAY 43-9006)	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
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. This compound 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. It 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
S7781	Sunitinib (SU-11248)	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 J Exp Clin Cancer Res, 2025, 44(1):290
S1490	Ponatinib (AP24534)	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 J Exp Clin Cancer Res, 2025, 44(1):290
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.	Nat Commun, 2025, 16(1):7853 CNS Neurosci Ther, 2025, 31(12):e70696 Sci Rep, 2025, 15(1):35889
S1029	Lenalidomide (CC-5013)	Lenalidomide is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.	Signal Transduct Target Ther, 2025, 10(1):29 Nat Commun, 2025, 16(1):3800 Cell Rep Med, 2025, S2666-3791(25)00102-8
S1264	PD173074	PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells.	Stem Cell Reports, 2025, 20(10):102640 Commun Biol, 2025, 8(1):125 Cell Stem Cell, 2024, S1934-5909(24)00294-7
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
S1018	Dovitinib (TKI-258)	Dovitinib (TKI-258, CHIR258) is a multitargeted RTK inhibitor, primarily targeting class III RTKs (FLT3/c-Kit) with IC50 values of 1 nM/2 nM. It is also potent against class IV (FGFR1/3) and class V (VEGFR1-4) RTKs, exhibiting IC50 values of 8–13 nM, while showing lower potency toward 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
S8064	Midostaurin (PKC412)	Midostaurin is a multi-targeted kinase inhibitor, including PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50 ranging from 80-500 nM.	Blood Adv, 2025, bloodadvances.2024015427 Onco Targets Ther, 2025, 18:489-501 Blood Cancer J, 2024, 14(1):207
S8401	Erdafitinib (JNJ-42756493)	Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. This compound 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
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
S2161	RAF265 (CHIR-265)	RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM in cell-free assays. This compound induces cell cycle arrest and apoptosis. Phase 2.	bioRxiv, 2025, 2025.04.29.651188 Cancer Cell, 2022, S1535-6108(22)00312-9 iScience, 2022, 25(10):105182
S7057	LY2874455	LY2874455 is a pan-FGFR inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM. Phase 1.	Cancer Drug Resist, 2025, 8:45 Cancer Discov, 2023, 13(9):1998-2011 Cancer Discov, 2023, 13(9):1998-2011
S1486	AEE788 (NVP-AEE788)	AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, respectively. It is less potent against VEGFR2/KDR, c-Abl, c-Src, and Flt-1, and does not inhibit Ins-R, IGF-1R, PKCα, or CDK1. This compound has reached Phase 1/2 clinical trials.	Cell Rep Med, 2022, 3(1):100492 Genome Med, 2020, 18;12(1):17 Oncotarget, 2019, 10(68):7185-7197
S1361	MGCD-265 analog	MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2.	Cancer Cell, 2022, S1535-6108(22)00312-9 Cell Rep Med, 2022, 3(1):100492 Protein Cell, 2019, 10(3):161-177
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. This compound 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
S1171	CYC116	CYC116 is a potent inhibitor of Aurora A/B with K_i of 8.0 nM/9.2 nM, is less potent to VEGFR2 (K_i of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1.	Sci Rep, 2024, 14(1):4303 Cell Chem Biol, 2023, 30(8):987-998.e24 Proc Natl Acad Sci U S A, 2022, 119(15):e2122512119
S2859	Golvatinib (E7050)	Golvatinib (E7050) is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, respectively. This compound does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM) and is currently in Phase 1/2 trials.	Int J Mol Sci, 2023, 24(11)9606 Int J Mol Sci, 2022, 23(23)14884 Cancer Sci, 2020, 111(10):3813-3823
S1220	OSI-930	OSI-930 is a potent inhibitor of Kit (c-Kit), KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; this compound is also potent to Flt-1, c-Raf and Lck and has low activity against PDGFRα/β, Flt-3 and Abl. Phase 1.	Nat Commun, 2024, 15(1):4739 Cell Rep, 2019, 28(9):2331-2344 Nat Biomed Eng, 2018, 2(8):578-588
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
S8573	Sitravatinib (MGCD516)	Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.	Commun Biol, 2025, 8(1):1185 Res Sq, 2025, rs.3.rs-6431257 JCI Insight, 2022, e148717
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
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.	Res Sq, 2025, rs.3.rs-7032881 bioRxiv, 2025, 2025.06.11.659120 Elife, 2023, 12e79840
S6412	Altiratinib	Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor of TRK, Met (c-Met), TIE2, and VEGFR2 kinases with IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. This compound inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM.	J Microbiol, 2025, 63(2):e2409001 Theranostics, 2021, 11(20):9918-9936 Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
S2201	BMS-794833	BMS-794833 is a potent ATP competitive inhibitor of Met (c-Met)/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378. Phase 1.	Cell Stem Cell, 2025, 32(11):1671-1690.e13 Cancer Res, 2021, canres.1428.2021
S0487	Sulfatinib	Sulfatinib is a potent and highly selective tyrosine kinase inhibitor against VEGFR1, VEGFR2, VEGFR3, FGFR1 and CSF1R with IC50 of 2 nM, 24 nM, 1 nM, 15 nM and 4 nM, respectively. This compound shows encouraging antitumor activity and manageable toxicities in patients with advanced NETs.	Front Oncol, 2023, 13:1158857
S2018	ENMD-2076 L-(+)-Tartaric acid	ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more selective for Aurora A than Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.
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
S8882	ODM-203	ODM-203 is a selective inhibitor of FGFR and VEGFR with ic50s of 11 nM,16 nM,6 nM, 35 nM,26 nM,9 nM,5 nM for recombinant FGFR1, FGFR2, FGFR3,FGFR4, VEGFR1, VEGFR2 and VEGFR3, respectively.
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.
E0499	4SC-203	4SC-203 (SC71710) is a multikinase inhibitor with potential antineoplastic activity. This compound selectively inhibits FMS-related tyrosine kinase 3 (FLT3/STK1), FLT3 mutated forms, and vascular endothelial growth factor receptors (VEGFRs).
S9621	Donafenib (Sorafenib D3)	Donafenib (Sorafenib D3, Bay 43-9006 D3, CM-4307) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 15 nM, 20 nM and 22 nM for Raf-1, mVEGFR-2, mVEGFR-3 and B-RAF, 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.
S6870	Ningetinib	Ningetinib (CT-053, DE-120, CT053PTSA) is a potent, orally bioavailable inhibitor of tyrosine kinase with IC50 of 6.7 nM, 1.9 nM and <1.0 nM for c-Met, VEGFR2 and Axl, respectively. This compound exhibits antitumor activity.
S6939	Nastorazepide	Nastorazepide (Z-360), a cholecystokinin-2/gastrin receptor (CCK2/gastrin receptor) antagonist, combines with gemcitabine prolonged survival and reduces gemcitabine-induced vascular endothelial growth factor (VEGF) expression in a pancreatic carcinoma orthotopic xenograft mouse.
E4914	Cabozantinib hydrochloride	Cabozantinib hydrochloride(XL184, BMS-907351 hydrochloride) is a potent small-molecule kinase inhibitor of c-MET and VEGFR2 with an IC50 of 1.3 nM, 0.035 nM respectively. It also inhibits RET, KIT, AXL, Tie2 and FLT3 with an IC50's of 5.2 nM, 4.6 nM, 7 nM, 14.3 nM, 11.3nM respectively. It can be promising agent for inhibiting tumor angiogenesis and metastasis in cancers with dysregulated MET and VEGFR signaling.
S4686	Vitamin E	Vitamin E (D-alpha-Tocopherol) is a fat-soluble vitamin with potent antioxidant properties. It is a potent peroxyl radical scavenger and inhibits noncompetitively cyclooxygenase activity in many tissues, also inhibits angiogenesis and tumor dormancy through suppressing vascular endothelial growth factor (VEGF) gene transcription.	Elife, 2025, 13RP94169 Cancer Drug Resist, 2025, 8:45 Signal Transduct Target Ther, 2024, 9(1):109
E0207	Chebulinic acid	Chebulinic acid, a phenolic compound isolated from Terminalia chebula fruit, is a novel Influenza viral neuraminidase inhibitor. This compound is a antiangiogenic agent through inhibiting the actions of VEGF. It shows antitumour activity.
S6809	SU5214	SU5214 is a inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 14.8 µM and EGFR with IC50 of 36.7 µm, respectively.
E1435	Tinengotinib	Tinengotinib (TT-00420) is a novel multiple kinase inhibitor that strongly inhibits Aurora A/B with IC50 values of 1.2/3.3 nM respectively. It also exhibits potent inhibitory activity on FGFR1/2/3, VEGFR1, JAK1/2, and CSF1R and can be used to treat several prominent signaling pathways in triple-negative breast cancer(TNBC).
E0142	XL092	XL092 (JUN04542) is an ATP-competitive inhibitor of multiple RTKs including MET, VEGFR2, AXL and MER, with IC50 values of 15 nM, 1.6 nM, 3.4 nM, and 7.2 nM in cell-based assays, respectively.

Signaling Pathway Map

Solid tumors require the growth and dissemination of blood vessels and lymphatic vessels to support the metastatic growth of cancers. Following the recognition of growth factor receptor pathways that regulate angiogenesis, a number of small molecular inhibitors and antibodies have been developed that target the activity of vascular endothelial growth factor (VEGF)-VEGF receptor (VEGFR) pathway. This includes oral small-molecule tyrosine kinase inhibitors currently in clinical practice, namely sunitinib and sorafenib. These are commonly used in the treatment algorithm for renal cell carcinoma (RCC) and hepatocellular carcinoma (HCC), two indications that are known to develop resistance to conventional chemotherapeutics.

The VEGFs include five known structurally-related mammalian ligands (VEGFA, VEGFB, VEGFC, VEGFD, and placenta growth factor, PLGF). The VEGFs are disulfide-bonded homodimers, however, VEGFA and PLGF heterodimers are also known to exist. Due to alternative splicing or due to processing, VEGF ligands occur as several different variants. As a result, these variants bind differently to both VEGFRs and to co-receptors resulting in different biological responses including angiogenesis, lymphangiogenesis, permeability, inflammatory cell recruitment and fatty acid uptake. VEGFs are produced by several different cell types and act in a paracrine manner. The VEGFs bind to three structurally related tyrosine kinases (VEGFR1, VEGFR2, and VEGFR3). Modulating the effect of the VEGFRs are a number of co-receptors that lack intrinsic catalytic activity (i.e. heparin sulfate, neurophilins and integrins) and bind to VEGF.^[1]

VEGFR1 (also known as Fms-like tyrosine kinase 1, Flt1, in mice) is a single-transmembrane glycoprotein structurally related to VEGFR2 and VEGFR3. VEGFR1 is expressed at high levels in vascular endothelial cells, and along with VEGFR2 binds to VEGFA. VEGFR1 is noted to bind exclusively to VEGFB and PIGF. Expression of VEGFR1 is noted to occur during vessel growth and remodeling activity. Non-endothelial cells that express VEGFR1 includes monocytes and macrophages, human tropholblasts, renal mesangial cells, vascular smooth muscle cells, dendritic cells and various tumor cells. A key regulator of VEGFR1 gene expression is hypoxia.^[1]

VEGFR2 (also known as KDR; kinase insert domain receptor, in the human and Flk1; fetal liver kinase-1, in mice) binds VEGFA with a 10-fold lower affinity than VEGFR1. Other targets of VEGFR2 include proteolytically processed VEGFC and VEGFD. The only known ligand to uniquely bind to VEGFR2 is the open reading frame-encoded VEGFE. VEGFR2 is expressed in most adult vascular endothelial cells as well as circulating endothelial progenitor cells, pancreatic duct cells, retinal progenitor cells, megakaryocytes and hematopoietic cells. VEGFR2 expression is induced in conjunction with active angiogenesis (i.e. the uterus during the reproductive cycle) and in pathological process related to neovascularization (i.e. cancer). VEGFR2, often in combination with VEGFR3, is expressed at significantly upregulated levels in the tumor vascular endothelium in most common human solid tumors. Tumor cells can also express VEGFR2, however, epithelial and mesenchymal tumor cells typically express VEGFR1 rather than VEGFR2. Nevertheless, increased expression of VEGFR2 on tumor cells has been noted for melanoma and hematological malignancies. And, there is evidence supporting a relationship between chronic inflammation and tumor development.^[1]

VEGFR3 (also known as Fms-like tyrosine kinase 4, Flt4 in the mouse) is activated by the binding of VEGFC or VEGFD, once these two ligands undergo proteolytic processing (this increases their affinity to VEGFR2 and VEGFR3). In addition, hVEGFD shows similar affinity to both VEGFR2 and VEGFR3, while mVEGFD binds only to VEGFR3. During embryogenesis, VEGFR3 expression occurs in the primary vascular plexus at day E8.5. In late stages of embryogenesis, VEGFR3 is expressed in venous endothelial cells of the cardinal vein, that results in VEGFR3-expressing lymphatics. Postnatally, VEGFR3 plays an important role in lymphatic endothelial cells, but its expression is also observed in endothelial cells engaged in active angiogenesis, such as tumor vessels, in endothelial tip cells of angiogenic sprouts in the developing retina or in chronic inflammatory wounds. The receptor is also found in non-endothelial cells such as osteoblasts, neuronal progenitors and macrophages – all of which may indirectly support angiogenesis. It remains unclear if tumor cells express VEGFR3. Despite this lack of clarity, inhibiting VEGFR3 activity is associated with the arrest of tumor vascularization, resulting in decreased vascular density in several tumor models.^[1]

Since the VEGF-VEGFR pathway plays a significant role in angiogenesis, and it is widely known that VEGF is highly expressed in tumor and stromal cells, especially in the inflammatory cells of human tumors, dozens of angiogenesis inhibitors are currently undergoing clinical trials.^[2] However, despite the number of compounds that has been identified for targeting the VEGF-VEGFR pathway, there is a high attrition rate. Several challenges in the development of angiogenesis inhibitors relate to their specificity, efficacy, side effects, and resistance to anti-angiogenic tumor therapy. However, the emergence of personalized medicine – based on the use of biomarkers – will likely lead to the identification of patient populations that is likely to define respondent groups.