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Inhibitors
| Cat.No. | Name | Information |
|---|---|---|
| M8949 | JI-101 | JI-101 is an orally available multi-kinase inhibitor of VEGFR2，PDGFRβ and EphB4 with potential antiangiogenic and antineoplastic activities. |
| M8917 | BAW2881 | BAW2881 (NVP-BAW2881) is a potent and selective VEGFR2 inhibitor with activity to inhibit chronic and acute skin inflammation. |
| M8916 | SU1498 | SU 1498 is a selective inhibitor of the receptor tyrosine kinase VEGF receptor 2 (VEGFR2, aka FLK1; IC50 = 700 nM). |
| M7573 | Avitinib maleate | Avitinib maleate is a pyrrolopyrimidine-based irreversible epidermal growth factor receptor (EGFR) inhibitor with an IC50 of 7.68 nM. |
| M7554 | Fruquintinib | Fruquintinib (HMPL-013) is a highly potent and selective VEGFR 1/2/3 inhibitor with IC50s of 33, 0.35, and 35 nM, respectively. |
| M7544 | SUN11602 | SUN11602 is a novel aniline compound with basic fibroblast growth factor-like activity. |
| M7530 | Anlotinib Dihydrochloride | Anlotinib Dihydrochloride is a novel multi-target tyrosine kinase inhibitor that is designed to primarily inhibit VEGFR2/3, FGFR1-4, PDGFRα/β, c-Kit, and Ret. |
| M6277 | Sunitinib | Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. |
| M6202 | 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 mutation, D816V in KIT Exon 17 (IC50 = 0.5 nM). |
| M6197 | Nintedanib Ethanesulfonate Salt | BIBF 1120 esylate is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively. |
| M5925 | Regorafenib HCl | Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, 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. |
| M5863 | Pazopanib HCl (GW786034 ) | 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. |
| M5592 | Dovitinib (TKI-258) Dilactic Acid | Dovitinib Dilactic acid (TKI258 Dilactic acid) is the Dilactic acid of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM. |
| M5342 | Toceranib | Toceranib(SU 11654; PHA 291639) is a kinase inhibitor with both antitumor and antiangiogenic activity through inhibition of KIT, vascular endothelial growth factor receptor 2, and PDGFRβ. |
| M5313 | 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. |
| M5005 | Regorafenib Monohydrate | Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, 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. |
| M3993 | SU4312 | SU4312 is a selective and potent inhibitor of VEGFR and PDGFR tyrosine kinases with IC50 values are 0.8 and 19.4 μM respectively. |
| M3792 | Vatalanib | Vatalanib is an inhibitor of the VEGFR tyrosine kinases VEGFR-1 (Flt-1, IC₅₀ = 77 nM) and VEGFR-2 (FLK-1/KDR, IC₅₀ = 37 nM), with slightly higher potency against the latter. |
| M3740 | ZM323881 | ZM323881 is a potent and selective VEGFR2 inhibitor with IC50 of 2 nM and almost has no activity on VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2. |
| M3678 | CEP-11981 | CEP-11981 is an oral vascular endothelial growth factor (VEGF) tyrosine kinase inhibitor. |
| M3269 | 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. |
| M3140 | ZM 323881 hydrochloride | ZM 323881 is a potent and selective VEGFR2 inhibitor with IC50 of <2 nM, almost no activity on VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2. |
| M3139 | ZM 306416 | ZM 306416 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. |
| M3097 | Tyrphostin AG 1296 | Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR. |
| M3096 | Tyrphostin 9 | Tyrphostin 9 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. |
| M3047 | TAK-593 | TAK-593 is a novel dual VEGFR/PDGFR inhibitor. |
| M3013 | SKLB1002 | SKLB1002 is a potent and ATP-competitive VEGFR2 inhibitor with IC50 of 32 nM. |
| M2194 | SU5402 | SU5402 is a potent and selective VEGFR and FGFR inhibitor with IC50 values of 0.02, 0.03, 0.51 and > 100 μM for VEGFR2, FGFR1, PDGFRβ and EGFR respectively. |
| M2153 | TSU-68 | TSU-68 (SU6668) is a protein kinase inhibitor of PDGF-Rβ, VEGF-R2 and FGF-R1 with IC50 of 0.06, 2.4 and 3.0 μM, respectively. |
| M2078 | SAR131675 | SAR131675 is a potent and selective VEGFR-3 inhibitor with IC50 of 20 nM. |
| M2074 | NVP-BHG712 | NVP-BHG712 is a very potent, selective inhbitor of the receptor tyrosine kinase EphB4 (ED50 = 25 nM). |
| M2031 | SU5416 | SU5416 is a novel small molecule multi-targeted kinase inhibitor of VEGF receptors, c-kit and FLT3. |
| M2011 | PP121 | PP121 is a dual inhibitor of tyrosine and phosphoinositide kinases. |
| M1999 | DMXAA | DMXAA (Vadimezan, ASA404) is a tumor-vascular disrupting agent (tumor-VDA) and competitive inhibitor of DT-diaphorase with Ki of 20 μM and IC50 of 62.5 μM, respectively. |
| M1995 | Ki8751 | Ki8751 is a potent, selective inhibitor of VEGFR-2 tyrosine kinase (IC50 = 0.9 nM). |
| M1994 | Telatinib | Telatinib (BAY 57-9352) is an orally active small-molecule tyrosine kinase inhibitor of VEGFR2, VEGFR3 and PDGFRβ with IC50 of 6 nM, 4 nM and 15 nM, respectively. |
| M1964 | Vandetanib | Vandetanib is a potent inhibitor of VEGFR (IC50 = 40 nM) and EGFR. |
| M1956 | Apatinib | Apatinib is a small-molecule multitargeted tyrosine kinase inhibitor of VEGFR2 with an IC50 of 2.43 nM. |
| M1944 | CP-547632 | CP-547632 is a novel VEGFR-2 tyrosine kinase inhibitor with IC50 of 11 nM. |
| M1941 | CP 673451 | CP 673451 is a potent inhibitor of platelet-derived growth factor beta-receptor (PDGFR-beta) with an IC50 of 1 nM. |
| M1936 | E-3810 | E-3810 is a novel small molecule inhibitor with potent and selective inhibitory activity of the Vascular Endothelial Growth Factor (VEGF) receptors 1-3 and of the Fibroblast Growth Factor (FGF) receptors 1-2. |
| M1920 | Motesanib Diphosphate | Motesanib (AMG 706) is a potent ATP-competitive inhibitor of VEGFR1/2/3, PDGFR, c-Kit and Ret with IC50 of 2 nM, 3 nM, 6 nM, 84 nM, 8 nM and 59 nM, respectively. |
| M1918 | Amuvatinib | Amuvatinib (MP470) is a novel receptor tyrosine kinase inhibitor that targets c-KIT and PDGFRα. |
| M1882 | Vatalanib dihydrochloride | Vatalanib is a selective small molecule protein kinase inhibitor of VEGF receptors 1-3. |
| M1842 | Pazopanib | Pazopanib is an oral angiogenesis inhibitor of tyrosine kinases, targeting vascular endothelial growth factor receptor, platelet-derived growth factor receptor, and c-Kit. |
| M1841 | Lenvatinib | Lenvatinib (E7080) is a potent inhibitor of multiple tyrosine kinases, including VEGF-R3 tyrosine kinase (IC50=5.2 nM) and VEGF-R2 tyrosine kinase (IC50=4.0 nM). |
| M1840 | BGJ398 | BGJ398 is a potent and selective FGFR kinase inhibitor with IC50 values of 0.9 nM, 1.4 nM, 1 nM and 60 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. |
| M1838 | Masitinib | Masitinib is a tyrosine kinase inhibitor targeting stem cell factor receptor (c-kit) and platelet-derived growth factor (PDGF) receptor. |
| M1827 | Sorafenib Tosylate | Sorafenib (BAY 43-9006) is an orally active multikinase inhibitor of tyrosine protein kinases VEGFR/PDGFR and RAF/MEK/ERK with IC50 values of 6, 22, 38 nM for Raf-1, wt BRAF and V599E mutant BRAF. |
| M1826 | Sunitinib Malate | Sunitinib is a multitargeted tyrosine kinase inhibitor of VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively. |
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