Home Protein Tyrosine Kinase -Angiogenesis VEGFR VEGFR2-선택적 Inhibitors

VEGFR2-선택적 Inhibitors

  • VEGFR1
  • VEGFR2
  • VEGFR3
Cat.No. 제품명 정보 선택적 / 팬 IC50 / Ki
S1119 Cabozantinib (XL184, BMS-907351) Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and 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, respectively. Selective VEGFR2/KDR, IC50: 0.035 nM
S4001 Cabozantinib malate (XL184) Cabozantinib malate is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and 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, respectively. Selective VEGFR2/KDR, IC50: 0.035 nM
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. Selective VEGFR2, IC50: 0.9 nM
S2221 Apatinib Apatinib is an orally bioavailable, selective VEGFR2 inhibitor with IC50 of 1 nM. Selective VEGFR2, IC50: 1 nM
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, respectively. Selective VEGFR2, IC50: 1.5 nM
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. Selective VEGFR2, IC50: <2 nM
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. Selective VEGFR2, IC50: 7 nM
S1040 Sorafenib Tosylate Sorafenib Tosylate (Bay 43-9006) is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively. Selective VEGFR2/Flk1, IC50: 15 nM; VEGFR2, IC50: 90 nM
S2201 BMS-794833 BMS-794833 is a potent ATP competitive inhibitor of 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. Selective VEGFR2, IC50: 15 nM
S2859 Golvatinib (E7050) Golvatinib (E7050) is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM). Phase 1/2. Selective VEGFR2, IC50: 16 nM
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. Phase 2. Selective VEGFR2, EC50: 30 nM
S7258 SKLB1002 SKLB1002 is a potent and ATP-competitive VEGFR2 inhibitor with IC50 of 32 nM. Selective VEGFR2, IC50: 32 nM
S1046 Vandetanib (ZD6474) Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM. Selective VEGFR2, IC50: 40 nM
S1171 CYC116 CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki 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. Selective VEGFR2, Ki: 44 nM
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, and also inhibits c-Kit. Selective VEGFR2, IC50: 80 nM
S7781 Sunitinib Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Selective VEGFR2 , IC50: 80 nM
S1264 PD173074 PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM, ~1000-fold selective for FGFR1 than PDGFR and c-Src. Selective VEGFR2, IC50: 100 nM-200 nM
S2845 Semaxanib (SU5416) Semaxanib (SU5416) is a potent and selective VEGFR(Flk-1/KDR) inhibitor with IC50 of 1.23 μM, 20-fold more selective for VEGFR than PDGFRβ, lack of activity against EGFR, InsR and FGFR. Phase 3. Selective VEGFR2/Flk1, IC50: 1.23 μM
S1470 TSU-68 (SU6668, Orantinib) TSU-68 (SU6668, Orantinib) has greatest potency against PDGFR autophosphorylation with Ki of 8 nM, 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. Selective Flk1, Ki: 2.1 μM
S1005 Axitinib Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM, respectively. Pan VEGFR2/Flk1, IC50: 0.18 nM; VEGFR2/KDR, IC50: 0.2 nM
S1017 Cediranib (AZD2171) Cediranib (AZD2171) 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, Phase 3. Pan VEGFR2/KDR, IC50: 0.5 nM
S1111 Foretinib (GSK1363089) Foretinib (GSK1363089) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met and KDR with IC50 of 0.4 nM and 0.9 nM. Less potent against Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2. Pan KDR, IC50: 0.86 nM
S1361 MGCD-265 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. Pan VEGFR2, IC50: 3 nM
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, ~10-fold more selective for VEGFR than PDGFR and Ret. Phase 3. Pan VEGFR2/Flk1, IC50: 6 nM; VEGFR2, IC50: 3 nM
S1003 Linifanib (ABT-869) Linifanib (ABT-869) 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). Phase 3. Pan VEGFR2/KDR, IC50: 4 nM
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. Phase 3. Pan VEGFR2/KDR, IC50: 4.0 nM
S1178 Regorafenib (BAY 73-4506) 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. Pan VEGFR2, IC50: 4.2 nM
S2231 Telatinib Telatinib 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. Pan VEGFR2, IC50: 6 nM
S1207 Tivozanib (AV-951) Tivozanib (AV-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. Pan VEGFR2, IC50: 6.5 nM
S1220 OSI-930 OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl. Phase 1. Pan KDR, IC50: 9 nM
S1010 Nintedanib (BIBF 1120) Nintedanib (BIBF 1120) 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. Phase 3. Pan VEGFR2, IC50: 13 nM
S7765 Dovitinib (TKI258) Lactate Dovitinib (TKI258) 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. Pan VEGFR2/Flk1, IC50: 13 nM
S1018 Dovitinib (TKI-258, CHIR-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. Phase 4. Pan VEGFR2/Flk1, IC50: 13 nM
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. Pan VEGFR2, IC50: 25 nM; Flk1, IC50: 89 nM
S1084 Brivanib (BMS-540215) Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. Phase 3. Pan VEGFR2, IC50: 25 nM; Flk1, IC50: 89 nM
S3012 Pazopanib Pazopanib 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, respectively. Pan VEGFR2, IC50: 30 nM
S1035 Pazopanib HCl (GW786034 HCl) Pazopanib (GW786034) 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, respectively. Pan VEGFR2, IC50: 30 nM
S1101 Vatalanib (PTK787) 2HCl Vatalanib (PTK787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 3. Pan VEGFR2/Flk1, IC50: 270 nM; VEGFR2/KDR, IC50: 37 nM
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. Pan VEGFR2/KDR, IC50: 58.2 nM
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 VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2. Pan VEGFR2/KDR, IC50: 58.2 nM
S1486 AEE788 (NVP-AEE788) AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2. Pan KDR, IC50: 77 nM
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. Pan VEGFR2, IC50: 160 nM