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Inhibitors
| Cat.No. | Name | Information |
|---|---|---|
| M10511 | TAS-115 mesylate | TAS-115 (Pamufetinib) mesylate inhibited the kinase activity of both VEGFR2 and MET and their signal-dependent cell growth as strongly as other known VEGFR or MET inhibitors. |
| M10329 | Ningetinib | Ningetinib is a potent, orally bioavailable tyrosine kinase inhibitor for Axl, VEGFR2 and c-Met with IC50 values of <1.0, 1.9 and 6.7 nM, respectively. |
| M9873 | Tanshinone IIA | Tanshinone IIA suppresses angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2. *The compound is unstable in solutions, freshly prepared is recommended. |
| M9757 | AC710 | AC710 is a potent, selective and orally active platelet-derived growth factor receptor-family (PDGFR) kinase inhibitor with potential anticancer activity. |
| M9626 | Sitravatinib | Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor. |
| M9540 | ODM-203 | ODM-203 is an orally available inhibitor of VEGFR and FGFR, with IC50s of 26, 9, 5 nM for VEGFR1, VEGFR2 and VEGFR3, and 11, 16, 6, 35 nM for recombinant FGFR1, FGFR2, FGFR3 and FGFR4, respectively. |
| M9465 | MAZ51 | MAZ51 is originally synthesized inhibitor of VEGFR-3 (Flt-4) tyrosine kinase, inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. |
| M9429 | SU14813 | SU14813 is a novel multiple receptor tyrosine kinase inhibitor with IC50s of 2, 50, 4, 15 nM for VEGFR-1, VEGFR-2, PDGFR-β and KIT. |
| M9285 | SU 5205 | SU 5205 is a VEGFR2 inhibitor with IC50 of 9.6 μM. |
| M9284 | SU-5408 | SU-5408 is a potent, cell-permeable inhibitor of mouse VEGFR2 kinase with IC50 of 70 nM. |
| M9283 | SU 5214 | SU 5214 is a modulator of tyrosine kinase signal transduction. |
| M9249 | BFH772 | BFH772 is a potent and selective VEGFR2 inhibitor with an IC50 value of 3 nM. |
| M9236 | Ranibizumab | Ranibizumab is a monoclonal antibody that inhibits angiogenesis by inhibiting Vascular endothelial growth factor A. |
| M9161 | NVP-ACC789 | NVP-ACC789 is an inhibitor of human VEGFR-1, VEGFR-2 (mouse VEGFR-2), VEGFR-3 and PDGFR-β with IC50s of 0.38, 0.02 (0.23), 0.18, 1.4 μM, respectively. |
| M9094 | EG00229 Trifluoroacetate salt | EG00229 Trifluoroacetate is the first small molecule inhibitor of the neuropilin-1 and VEGF-A interaction with an IC50 of inhibition of 8 uM (125I-VEGF binding to PAE/NRP1 cells). |
| M9073 | Apatinib | Apatinib is a selective VEGFR2 inhibitor with IC50 of 1 nM. |
| 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). |
| M8758 | GW806742X | GW806742X is an ATP site-targeing kinase inhibitor (IC50 in nM = 2/VEGFR2, 15/SRC, 47/C-FMS, 851/GSK3, 9016/ERBB2, 9120/FGFR) with potent antiproliferation activity against cancer cultures (IC50 in nM = 5/HUVEC-v, 424/HUVEC-b, 81/HEF, 453/MDA468, 470/A375P, 693/HT29, 734/PC3), GW806742X is now better known as Compound 1 for its anti-necroptosis activity via affinity interaction with ML |
| M8512 | EG00229 | EG00229 is an antagonist of the VEGF-A receptor neuropilin 1 (NRP1), which decreases viability of A549 lung carcinoma cells. |
| M8434 | R1530 | R1530 is a multi-kinase inhibitor with activity against several kinases associated with tumor growth and angiogenesis, including VEGFR, FGFR, PDGFR, Chk2 and Cdk2. |
| 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. |
| 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 | 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 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. |
| M6166 | Bevacizumab | Humanized vascular endothelial growth factor (VEGF) antibody (bevacizumab; Avastin) is a highly effective monoclonal antibody against metastatic colorectal cancer and several other advanced late stage cancers. |
| 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. |
| M3849 | Aflibercept | Aflibercept is an inhibitor of vascular endothelial growth factor (VEGF). |
| 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 (Orantinib) | 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. |
| M2139 | Sulfatinib | Sulfatinib is an orally bioavailable, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3, and the fibroblast growth factor receptor type 1 (FGFR1). |
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