E0050New |
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.
|
|
|
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. |
-
Adv Sci (Weinh), 2021, e2101848
|
|
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. |
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Cell Rep Med, 2022, 3(1):100492
-
Cancer Lett, 2021, 507:80-88
|
|
S1005 |
Axitinib (AG 013736)
|
Axitinib (AG 013736) 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, 2022, S1535-6108(21)00662-0
-
Sci Adv, 2022, 8(6):eabg9455
-
Sci Adv, 2022, 8(2):eabi8683
|
|
S1010 |
Nintedanib (BIBF 1120)
|
Nintedanib (BIBF 1120, Intedanib, Vargatef, Ofev) 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. |
-
Theranostics, 2022, 12(2):747-766
-
Drug Des Devel Ther, 2022, 16:397-411
-
Integr Biol (Camb), 2022, 14(1):1-12
|
|
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. |
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Cell Rep Med, 2022, 3(1):100492
-
Front Oncol, 2021, 11:763895
|
|
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. |
-
Cell Rep Med, 2022, 3(1):100492
-
Mol Cell, 2021, S1097-2765(21)00507-4
-
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
|
|
S1026 |
Imatinib (STI571) Mesylate
|
Imatinib (STI571, CGP057148B, Gleevec) 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. |
-
Signal Transduct Target Ther, 2022, 7(1):33
-
Sci Adv, 2022, 8(6):eabg9455
-
Osteoarthritis Cartilage, 2022, S1063-4584(22)00035-8
|
|
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
-
Drug Metab Dispos, 2021, 49(1):53-61
-
Cell Stem Cell, 2019, 25(1):69-86
|
|
S1035 |
Pazopanib HCl (GW786034 HCl)
|
Pazopanib HCl (GW786034 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. |
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Cancer Cell, 2021, S1535-6108(21)00659-0
-
Cancers (Basel), 2021, 13(14)3635
|
|
S1040 |
Sorafenib (BAY 43-9006) tosylate
|
Sorafenib (BAY 43-9006) 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. |
-
Cancer Cell, 2022, S1535-6108(21)00662-0
-
Proc Natl Acad Sci U S A, 2022, 119(10):e2107453119
-
Cancer Metab, 2022, 10(1):4
|
|
S1042 |
Sunitinib (SU11248) malate
|
Sunitinib (SU11248) 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. |
-
Clin Cancer Res, 2022, clincanres.4291.2021
-
Cancers (Basel), 2022, 14(4)903
-
Biomedicines, 2022, 10(2)321
|
|
S1064 |
Masitinib (AB1010)
|
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. |
-
Vet Comp Oncol, 2022, 10.1111/vco.12817
-
Cell Chem Biol, 2021, S2451-9456(21)00303-2
-
Drug Metab Dispos, 2021, 49(1):53-61
|
|
S1111 |
Foretinib (GSK1363089)
|
Foretinib (GSK1363089, EXEL-2880, XL-880, GSK089) 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. |
-
Int J Mol Sci, 2022, 23(2)775
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Cell Rep Med, 2022, 3(1):100492
|
|
S1164 |
Lenvatinib (E7080)
|
Lenvatinib (E7080) 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. |
-
Clin Transl Med, 2022, 12(1):e662
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Nature, 2021, 595(7869):730-734
|
|
S1178 |
Regorafenib (BAY 73-4506)
|
Regorafenib (BAY 73-4506, Fluoro-Sorafenib, Resihance, Stivarga) 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. |
-
Cancer Cell, 2022, S1535-6108(21)00662-0
-
Cell Rep, 2022, 38(10):110490
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
|
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. |
-
Cell, 2021, 184(2):334-351.e20
-
Sci Adv, 2021, 7(4)eabd7851
-
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
|
|
S1207 |
Tivozanib (AV-951)
|
Tivozanib (AV-951, KRN-951) 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. |
-
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Hum Cell, 2021, 10.1007/s13577-021-00639-4
|
|
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. |
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
mBio, 2021, 12(6):e0322821
-
Hum Cell, 2021, 34(6):1911-1918
|
|
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. |
-
Front Oncol, 2021, 11:650052
-
J Clin Med, 2020, 9(3)
-
Front Pharmacol, 2020, 11:572624
|
|
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. |
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Hum Cell, 2021, 34(6):1911-1918
-
Hum Cell, 2021, 10.1007/s13577-021-00639-4
|
|
S1490 |
Ponatinib (AP24534)
|
Ponatinib (AP24534) 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. |
-
J Immunother Cancer, 2022, 10(1)e003766
-
JCI Insight, 2022, 7(7)e154824
-
Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287
|
|
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. |
-
Lab Invest, 2021, 10.1038/s41374-021-00704-4
-
Oncol Rep, 2021, 45(1):83-94
-
Oncol Lett, 2021, 22(1):537
|
|
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
|
|
S2475 |
Imatinib (STI571)
|
Imatinib (STI571, CGP057148B, Gleevec) 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. |
-
Sci Adv, 2022, 8(6):eabg9455
-
Osteoarthritis Cartilage, 2022, S1063-4584(22)00035-8
-
J Oncol, 2022, 2022:4112016
|
|
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
-
Biochem Biophys Res Commun, 2015, 465(1):137-44
|
|
S2730 |
Crenolanib (CP-868596)
|
Crenolanib (CP-868596, ARO 002) 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. |
-
Mol Cancer Ther, 2022, OF1-OF11
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Cell Rep Med, 2022, 3(1):100492
|
|
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
|
|
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
|
|
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. |
-
J Pharmacol Exp Ther, 2022, 380(2):114-125
-
Birth Defects Res, 2022, 10.1002/bdr2.2001
-
Cancer Res, 2021, canres.1222.2021
|
|
S4018 |
Sennoside B
|
Sennoside B, a kind of irritant laxative isolated from rhei rhizome, inhibits PDGF-stimulated cell proliferation. |
|
|
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. |
-
ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
-
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
-
Front Oncol, 2021, 11:796839
|
|
S5077 |
Regorafenib (BAY-734506) Monohydrate
|
Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) 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. |
-
Pharmazie, 2022, 77(2):54-58
-
ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
-
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
|
|
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. |
-
Theranostics, 2022, 12(2):747-766
-
Integr Biol (Camb), 2022, 14(1):1-12
-
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
|
|
S5240 |
Lenvatinib (E7080) Mesylate
|
Lenvatinib Mesylate (E7080) 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. |
-
Clin Transl Med, 2022, 12(1):e662
-
Pharmazie, 2022, 77(2):54-58
-
J Immunother Cancer, 2021, 9(6)e002305
|
|
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. |
|
|
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. |
|
|
S6843 |
X-82 (Vorolanib)
|
X-82 (Vorolanib, 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. |
|
|
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
|
|
S7397 |
Sorafenib (BAY 43-9006)
|
Sorafenib (BAY 43-9006, NSC-724772) 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. |
-
Proc Natl Acad Sci U S A, 2022, 119(10):e2107453119
-
Cell Mol Life Sci, 2022, 79(5):228
-
Int J Mol Sci, 2022, 23(8)4277
|
|
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.
|
-
Nature, 2021, 10.1038/s41586-020-03085-8
-
Nat Commun, 2021, 12(1):2551
-
Proc Natl Acad Sci U S A, 2021, 118(20)e2100342118
|
|
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. |
|
|
S7765 |
Dovitinib (TKI258) Lactate
|
Dovitinib (TKI258, CHIR258) Lactate 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
|
|
S7781 |
Sunitinib (SU11248)
|
Sunitinib (SU11248) 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. |
-
Mol Cell, 2022, S1097-2765(22)00105-8
-
Clin Cancer Res, 2022, clincanres.4291.2021
-
Cancers (Basel), 2022, 14(4)903
|
|
S8015 |
Agerafenib (RXDX-105)
|
Agerafenib (RXDX-105, 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
-
Photodermatol Photoimmunol Photomed, 2019, 10.1111/phpp.12520
|
|
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. |
-
J Cardiovasc Dev Dis, 2021, 8(3)28
-
Mol Med Rep, 2021, 23(4):1
-
CellPress, 2021, None
|
|
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. |
-
J Cell Sci, 2021, jcs.258685
-
Molecules, 2020, 8;25(9) pii: E2220
|
|
S8401 |
Erdafitinib (JNJ-42756493)
|
Erdafitinib (JNJ-42756493) 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. |
-
JCI Insight, 2022, 7(7)e154824
-
Oncoimmunology, 2022, 11(1):2021619
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
|
S8553 |
Avapritinib (BLU-285)
|
Avapritinib (BLU-285) 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). |
-
Sci Adv, 2022, 8(6):eabg9455
-
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
-
JCI Insight, 2020, 143474
|
|
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. |
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S8757 |
Ripretinib (DCC-2618)
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DCC-2618 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. |
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Cancers (Basel), 2021, 13(15)3699
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J Pers Med, 2020, 10(4)E234
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Expert Opin Pharmacother, 2019, 20(13):1539-1550
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S8780 |
AZD3229
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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). |
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S9973New |
Flumatinib (HH-GV-678)
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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.
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S4736 |
Trapidil
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Trapidil (Rocornal, Trapymin, Avantrin, Trapymine) is a PDGF antagonist that can inhibit the proliferation of the PDGF-producing glioma cells. |
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Hum Cell, 2022, 10.1007/s13577-022-00671-y
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Curr Issues Mol Biol, 2021, 43(3):1726-1740
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Hum Cell, 2021, 10.1007/s13577-021-00579-z
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E0050New |
Seralutinib (GB002)
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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.
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S0504 |
SU14813
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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. |
- Adv Sci (Weinh), 2021, e2101848
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S1003 |
Linifanib (ABT-869)
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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. |
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Cell Rep Med, 2022, 3(1):100492
- Cancer Lett, 2021, 507:80-88
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S1005 |
Axitinib (AG 013736)
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Axitinib (AG 013736) 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, 2022, S1535-6108(21)00662-0
- Sci Adv, 2022, 8(6):eabg9455
- Sci Adv, 2022, 8(2):eabi8683
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S1010 |
Nintedanib (BIBF 1120)
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Nintedanib (BIBF 1120, Intedanib, Vargatef, Ofev) 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. |
- Theranostics, 2022, 12(2):747-766
- Drug Des Devel Ther, 2022, 16:397-411
- Integr Biol (Camb), 2022, 14(1):1-12
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S1017 |
Cediranib (AZD2171)
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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. |
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Cell Rep Med, 2022, 3(1):100492
- Front Oncol, 2021, 11:763895
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S1018 |
Dovitinib (TKI-258)
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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. |
- Cell Rep Med, 2022, 3(1):100492
- Mol Cell, 2021, S1097-2765(21)00507-4
- Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
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S1026 |
Imatinib (STI571) Mesylate
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Imatinib (STI571, CGP057148B, Gleevec) 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. |
- Signal Transduct Target Ther, 2022, 7(1):33
- Sci Adv, 2022, 8(6):eabg9455
- Osteoarthritis Cartilage, 2022, S1063-4584(22)00035-8
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S1032 |
Motesanib Diphosphate (AMG-706)
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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
- Drug Metab Dispos, 2021, 49(1):53-61
- Cell Stem Cell, 2019, 25(1):69-86
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S1035 |
Pazopanib HCl (GW786034 HCl)
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Pazopanib HCl (GW786034 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. |
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Cancer Cell, 2021, S1535-6108(21)00659-0
- Cancers (Basel), 2021, 13(14)3635
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S1040 |
Sorafenib (BAY 43-9006) tosylate
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Sorafenib (BAY 43-9006) 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. |
- Cancer Cell, 2022, S1535-6108(21)00662-0
- Proc Natl Acad Sci U S A, 2022, 119(10):e2107453119
- Cancer Metab, 2022, 10(1):4
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S1042 |
Sunitinib (SU11248) malate
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Sunitinib (SU11248) 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. |
- Clin Cancer Res, 2022, clincanres.4291.2021
- Cancers (Basel), 2022, 14(4)903
- Biomedicines, 2022, 10(2)321
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S1064 |
Masitinib (AB1010)
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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. |
- Vet Comp Oncol, 2022, 10.1111/vco.12817
- Cell Chem Biol, 2021, S2451-9456(21)00303-2
- Drug Metab Dispos, 2021, 49(1):53-61
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S1111 |
Foretinib (GSK1363089)
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Foretinib (GSK1363089, EXEL-2880, XL-880, GSK089) 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. |
- Int J Mol Sci, 2022, 23(2)775
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Cell Rep Med, 2022, 3(1):100492
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S1164 |
Lenvatinib (E7080)
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Lenvatinib (E7080) 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. |
- Clin Transl Med, 2022, 12(1):e662
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Nature, 2021, 595(7869):730-734
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S1178 |
Regorafenib (BAY 73-4506)
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Regorafenib (BAY 73-4506, Fluoro-Sorafenib, Resihance, Stivarga) 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. |
- Cancer Cell, 2022, S1535-6108(21)00662-0
- Cell Rep, 2022, 38(10):110490
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
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S1181 |
ENMD-2076
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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. |
- Cell, 2021, 184(2):334-351.e20
- Sci Adv, 2021, 7(4)eabd7851
- J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
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S1207 |
Tivozanib (AV-951)
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Tivozanib (AV-951, KRN-951) 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. |
- Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Hum Cell, 2021, 10.1007/s13577-021-00639-4
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S1244 |
Amuvatinib (MP-470)
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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. |
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- mBio, 2021, 12(6):e0322821
- Hum Cell, 2021, 34(6):1911-1918
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S1363 |
Ki8751
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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. |
- Front Oncol, 2021, 11:650052
- J Clin Med, 2020, 9(3)
- Front Pharmacol, 2020, 11:572624
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S1470 |
Orantinib (SU6668)
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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. |
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Hum Cell, 2021, 34(6):1911-1918
- Hum Cell, 2021, 10.1007/s13577-021-00639-4
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S1490 |
Ponatinib (AP24534)
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Ponatinib (AP24534) 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. |
- J Immunother Cancer, 2022, 10(1)e003766
- JCI Insight, 2022, 7(7)e154824
- Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287
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S1536 |
CP-673451
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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. |
- Lab Invest, 2021, 10.1038/s41374-021-00704-4
- Oncol Rep, 2021, 45(1):83-94
- Oncol Lett, 2021, 22(1):537
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S2231 |
Telatinib
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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
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S2475 |
Imatinib (STI571)
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Imatinib (STI571, CGP057148B, Gleevec) 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. |
- Sci Adv, 2022, 8(6):eabg9455
- Osteoarthritis Cartilage, 2022, S1063-4584(22)00035-8
- J Oncol, 2022, 2022:4112016
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S2622 |
PP121
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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
- Biochem Biophys Res Commun, 2015, 465(1):137-44
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S2730 |
Crenolanib (CP-868596)
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Crenolanib (CP-868596, ARO 002) 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. |
- Mol Cancer Ther, 2022, OF1-OF11
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Cell Rep Med, 2022, 3(1):100492
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S2774 |
MK-2461
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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
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S2895 |
Tyrphostin 9
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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
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S3012 |
Pazopanib
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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. |
- J Pharmacol Exp Ther, 2022, 380(2):114-125
- Birth Defects Res, 2022, 10.1002/bdr2.2001
- Cancer Res, 2021, canres.1222.2021
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S4018 |
Sennoside B
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Sennoside B, a kind of irritant laxative isolated from rhei rhizome, inhibits PDGF-stimulated cell proliferation. |
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S4947 |
Regorafenib Hydrochloride
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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. |
- ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
- Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
- Front Oncol, 2021, 11:796839
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S5077 |
Regorafenib (BAY-734506) Monohydrate
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Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) 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. |
- Pharmazie, 2022, 77(2):54-58
- ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
- Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
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S5234 |
Nintedanib Ethanesulfonate Salt
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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. |
- Theranostics, 2022, 12(2):747-766
- Integr Biol (Camb), 2022, 14(1):1-12
- Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
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S5240 |
Lenvatinib (E7080) Mesylate
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Lenvatinib Mesylate (E7080) 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. |
- Clin Transl Med, 2022, 12(1):e662
- Pharmazie, 2022, 77(2):54-58
- J Immunother Cancer, 2021, 9(6)e002305
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S5272 |
Toceranib phosphate
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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. |
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S6526 |
SKLB 610
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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. |
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S6843 |
X-82 (Vorolanib)
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X-82 (Vorolanib, 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. |
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S7003 |
AZD2932
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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.
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- Cancer Res, 2020, canres.1992.2020
- Molecules, 2020, 8;25(9) pii: E2220
- Development, 2016, 143(23):4394-4404
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S7397 |
Sorafenib (BAY 43-9006)
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Sorafenib (BAY 43-9006, NSC-724772) 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. |
- Proc Natl Acad Sci U S A, 2022, 119(10):e2107453119
- Cell Mol Life Sci, 2022, 79(5):228
- Int J Mol Sci, 2022, 23(8)4277
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S7667 |
SU5402
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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.
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- Nature, 2021, 10.1038/s41586-020-03085-8
- Nat Commun, 2021, 12(1):2551
- Proc Natl Acad Sci U S A, 2021, 118(20)e2100342118
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S7688 |
Ki20227
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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. |
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S7765 |
Dovitinib (TKI258) Lactate
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Dovitinib (TKI258, CHIR258) Lactate 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.
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- Mol Cell, 2021, S1097-2765(21)00507-4
- Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
- Cancer Res, 2021, canres.1780.2020
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S7781 |
Sunitinib (SU11248)
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Sunitinib (SU11248) 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. |
- Mol Cell, 2022, S1097-2765(22)00105-8
- Clin Cancer Res, 2022, clincanres.4291.2021
- Cancers (Basel), 2022, 14(4)903
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S8015 |
Agerafenib (RXDX-105)
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Agerafenib (RXDX-105, 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
- Photodermatol Photoimmunol Photomed, 2019, 10.1111/phpp.12520
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S8024 |
Tyrphostin AG 1296
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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. |
- J Cardiovasc Dev Dis, 2021, 8(3)28
- Mol Med Rep, 2021, 23(4):1
- CellPress, 2021, None
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S8161 |
ON123300
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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. |
- J Cell Sci, 2021, jcs.258685
- Molecules, 2020, 8;25(9) pii: E2220
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S8401 |
Erdafitinib (JNJ-42756493)
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Erdafitinib (JNJ-42756493) 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. |
- JCI Insight, 2022, 7(7)e154824
- Oncoimmunology, 2022, 11(1):2021619
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
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S8553 |
Avapritinib (BLU-285)
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Avapritinib (BLU-285) 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). |
- Sci Adv, 2022, 8(6):eabg9455
- Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
- JCI Insight, 2020, 143474
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S8721 |
PDGFR inhibitor 1
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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. |
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S8757 |
Ripretinib (DCC-2618)
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DCC-2618 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. |
- Cancers (Basel), 2021, 13(15)3699
- J Pers Med, 2020, 10(4)E234
- Expert Opin Pharmacother, 2019, 20(13):1539-1550
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S8780 |
AZD3229
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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). |
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S9973New |
Flumatinib (HH-GV-678)
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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.
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