VEGFR

VEGFR Inhibitors (46)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
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 in cell-free assays, respectively.
  • Hepatology, 2013, 59(4):1435-47
  • Blood, 2013, 122(9):1621-33
  • Blood, 2012, 120(19):4104-15
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.
  • Nature, 2011, 478(7369):349-55
  • Sci Transl Med, 2015, 7(284):284ra57
  • Cell Res, 2011, 21(7):1080-7
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 in cell-free assays, respectively.
  • Cancer Discov, 2014, 4(7):816-27
  • Nat Commun, 2014, 5:3116
  • Mol Cancer Ther, 2014, 10.1158/1535-7163.MCT-14-0274
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.
  • Nature, 2015, 10.1038/nature14329
  • Cancer Cell, 2012, 22(5):656-67
  • Sci Transl Med, 2014, 6(261):261ra152
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 in Porcine aorta endothelial cells, respectively.
  • Cancer Discov, 2012, 2(4):344-55
  • Development, 2013, 140(20):4214-25
  • Anal Chem, 2014, 86(17):8842-9
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.
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.
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.
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.
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 in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2.
  • Nat Genet, 2012, 44(8):852-60
  • Leukemia, 2014, 28(3):629-41
  • Cancer Res, 2011, 71(15):5255-64
S1046 Vandetanib (ZD6474) Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay.
  • Nature, 2015, 10.1038/nature14329
  • Nat Commun, 2014, 5:3116
  • Hypertension, 2011, 58(1):85-92
S7258 SKLB1002 SKLB1002 is a potent and ATP-competitive VEGFR2 inhibitor with IC50 of 32 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.
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.
  • Mol Cell Proteomics, 2012, 11(9):745-57
  • Sci Rep, 2015, 5:7890
S2221 Apatinib Apatinib is an orally bioavailable, selective VEGFR2 inhibitor with IC50 of 1 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.
  • Prostate, 2013, 73(13):1453-61
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.
  • J Med Chem, 2015,
  • J Chem Inf Model, 2014, 54(3):881-93
  • Cell Physiol Biochem, 2013, 32(5):1541-50
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.
  • Int J Oncol, 2014, 44(3):959-69
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 in cell-free assays. Phase 4.
  • Cancer Res, 2013, 73(16):5195-205
  • Haematologica, 2011, 96(6):922-6
  • Expert Opin Investig Drugs, 2014, 23(4):469-87
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.
  • Cancer Res, 2013, 73(20):6310-22
  • Vet Comp Oncol, 2013, 10.1111/vco.12046
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. Phase 3.
  • PLoS One, 2013, 8(5):e64369
  • Asian Pac J Cancer Prev, 2014, 5(7):3113-21
  • Chin J Cancer Res, 2013, 25(5):572-84
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.
  • Biochem Pharmacol, 2012, 84(6):766-74
  • BMC Microbiol, 2013, 13(1):249
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 in cell-free assays, respectively.
  • Cancer Discov, 2013, 3(6):636-47
  • J Virol, 2011, 85(5):2296-303
  • Expert Opin Pharmacother, 2014, 15(11):1489-99
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. Phase 2.
  • Hepatology, 2012, 56(6):2363-74
  • Mol Cell Proteomics, 2012, 11(6):M112.017764
  • Pigment Cell Melanoma Res, 2014, 27(1):124-33
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.
  • Cancer Res, 2013, 73(20):6310-22
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.
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.
  • Science, 2011, 331(6019):912-6
  • Cancer Discov, 2013, 3(6):636-47
  • Gut, 2014, 63(12):1932-42
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 in cell-free assays, respectively.
  • J Virol, 2011, 85(5):2296-303
  • Clin Cancer Res, 2014, 19(9):2368-80
  • Expert Opin Pharmacother, 2014, 15(11):1489-99
S1101 Vatalanib (PTK787) 2HCl Vatalanib (PTK787) 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 Biotechnol, 2013, 31(10):898-907
  • J Clin Invest, 2011, 121(8):3005-23
  • Cell Res, 2011, 21(7):1080-7
S2769 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, 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.
  • Haematologica, 2011, 96(6):922-6
  • Expert Opin Investig Drugs, 2014, 23(4):469-87
  • Br J Cancer, 2011, 104(1):75-82
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 in HUVEC cell line, Phase 3.
  • Cancer Res, 2013, 73(16):5195-205
  • Clin Cancer Res, 2014, 20(14):3849-61
  • Mol Cancer Ther, 2013, 12(12):2909-16
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 in cell-free assays, respectively.
  • J Clin Endocrinol Metab, 2013, 98(6):2502-12
  • Cell Death Dis, 2014, 5:e1278
  • Mol Pharmacol, 2013, 84(4):562-71
S1470 TSU-68 (SU6668, Orantinib) TSU-68 (SU6668, Orantinib) 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.
  • Proc Natl Acad Sci U S A, 2014, 111(44):E4706-15
  • Mol Cell Proteomics, 2012, 11(9):745-57
  • J Biol Chem, 2014, 289(19):13026-41
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.
  • Cancer Lett, 2013, 340(1):43-50
S2842 SAR131675 SAR131675 is a VEGFR3 inhibitor with IC50/Ki 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.
  • Hum Mol Genet, 2015, 24(4):926-38
  • Neuroscience, 2015, 290C:90-102
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.
  • OncoImmunology, 2015, 10.1080/2162402X.2014.998107
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.
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.
S2897 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.
  • Sci Rep, 2015, 5:7890
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 in cell-free assays, respectively.
  • Cell Death Dis, 2013, 4:e627
  • Mol Imaging, 2014, 13(0):1-5
  • Genes Genomics, 2014, 36(6):829-841
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.
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.
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.
  • Mol Cell Proteomics, 2012, 11(6):M112
  • Liver Int, 2011, 32(3):400-9
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 in cell-free assays. Phase 3.
  • Nature, 2011, 478(7369):349-55
  • Nat Neurosci, 2014, 17(1):24-6
  • Cell Death Differ, 2010, 17(9):1381-91
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.
  • International Journal of Cardiology, 2015, 183C:221-231
  • Cardiovasc Res, 2011, 91(3):402-11
  • Mol Cell Endocrinol, 2013, 377(1-2):1-6
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.
  • Biochem Pharmacol, 2014, 89(1):52-61

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1040 Sorafenib Tosylate 0.01 mg/mL 127 mg/mL <1 mg/mL
S1042 Sunitinib Malate <1 mg/mL 15 mg/mL <1 mg/mL
S1119 Cabozantinib (XL184, BMS-907351) <1 mg/mL 100 mg/mL <1 mg/mL
S1490 Ponatinib (AP24534) <1 mg/mL 30 mg/mL <1 mg/mL
S1005 Axitinib <1 mg/mL 35 mg/mL <1 mg/mL
S7003 AZD2932 <1 mg/mL 89 mg/mL 5 mg/mL
S7781 Sunitinib <1 mg/mL 79 mg/mL 13 mg/mL
S7765 Dovitinib (TKI258) Lactate 66 mg/mL 100 mg/mL 1 mg/mL
S7057 LY2874455 <1 mg/mL 88 mg/mL 88 mg/mL
S1111 Foretinib (GSK1363089) <1 mg/mL 127 mg/mL <1 mg/mL
S1046 Vandetanib (ZD6474) <1 mg/mL 4 mg/mL <1 mg/mL
S7258 SKLB1002 <1 mg/mL 7 mg/mL <1 mg/mL
S2201 BMS-794833 <1 mg/mL 94 mg/mL <1 mg/mL
S1363 Ki8751 <1 mg/mL 47 mg/mL <1 mg/mL
S2221 Apatinib <1 mg/mL 22 mg/mL <1 mg/mL
S1486 AEE788 (NVP-AEE788) <1 mg/mL 88 mg/mL <1 mg/mL
S1207 Tivozanib (AV-951) <1 mg/mL 20 mg/mL <1 mg/mL
S1084 Brivanib (BMS-540215) <1 mg/mL 74 mg/mL 3 mg/mL
S1018 Dovitinib (TKI-258, CHIR-258) <1 mg/mL 30 mg/mL <1 mg/mL
S1181 ENMD-2076 1 mg/mL 105 mg/mL <1 mg/mL
S1164 Lenvatinib (E7080) <1 mg/mL 40 mg/mL <1 mg/mL
S1220 OSI-930 <1 mg/mL 89 mg/mL 3 mg/mL
S1035 Pazopanib HCl (GW786034 HCl) <1 mg/mL 17 mg/mL <1 mg/mL
S2161 RAF265 (CHIR-265) <1 mg/mL 100 mg/mL 33 mg/mL
S1171 CYC116 <1 mg/mL 24 mg/mL <1 mg/mL
S1138 Brivanib Alaninate (BMS-582664) <1 mg/mL 88 mg/mL 88 mg/mL
S1264 PD173074 <1 mg/mL 100 mg/mL 100 mg/mL
S3012 Pazopanib <1 mg/mL 88 mg/mL <1 mg/mL
S1101 Vatalanib (PTK787) 2HCl 10 mg/mL 85 mg/mL 6 mg/mL
S2769 Dovitinib (TKI-258) Dilactic Acid 70 mg/mL 90 mg/mL <1 mg/mL
S1017 Cediranib (AZD2171) <1 mg/mL 90 mg/mL <1 mg/mL
S1178 Regorafenib (BAY 73-4506) <1 mg/mL 97 mg/mL <1 mg/mL
S1470 TSU-68 (SU6668, Orantinib) <1 mg/mL 62 mg/mL <1 mg/mL
S1361 MGCD-265 <1 mg/mL 104 mg/mL <1 mg/mL
S2842 SAR131675 <1 mg/mL 30 mg/mL <1 mg/mL
S2845 Semaxanib (SU5416) <1 mg/mL 22 mg/mL 2 mg/mL
S2896 ZM 323881 HCl <1 mg/mL 10 mg/mL <1 mg/mL
S2859 Golvatinib (E7050) <1 mg/mL 20 mg/mL <1 mg/mL
S2897 ZM 306416 <1 mg/mL 67 mg/mL <1 mg/mL
S4001 Cabozantinib malate (XL184) <1 mg/mL 100 mg/mL <1 mg/mL
S1557 KRN 633 <1 mg/mL 9 mg/mL <1 mg/mL
S1003 Linifanib (ABT-869) <1 mg/mL 75 mg/mL <1 mg/mL
S1010 Nintedanib (BIBF 1120) <1 mg/mL 6 mg/mL 3 mg/mL
S1032 Motesanib Diphosphate (AMG-706) 19 mg/mL 100 mg/mL <1 mg/mL
S2231 Telatinib <1 mg/mL 82 mg/mL 1 mg/mL
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