FGFR

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FGFR Inhibitors (14)

water-soluble

Cat.No. Product Name Information Product Citations Customer Reviews
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.
  • Cancer Cell, 2012, 22(5):656-67
  • Proc Natl Acad Sci U S A, 2014, 10.1073/pnas.1321173111
  • Cancer Res, 2013, 73(16):5195-205
S2183 BGJ398 (NVP-BGJ398) BGJ398 (NVP-BGJ398) is a potent and selective FGFR inhibitor for FGFR1/2/3 with IC50 of 0.9 nM/1.4 nM/1 nM, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. Phase 2.
  • Hepatology, 2013, 10.1002/hep.26890
  • J Cell Physiol, 2014, 10.1002/jcp.24610
  • Cancer Sci, 2013, 104(12):1618-25
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.
  • Nature, 2011, 478(7369):349-55
  • Cell Death Differ, 2010, 17(9):1381-91
  • Mol Cancer Ther, 2013, 12(9):1749-62
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.
  • Science, 2011, 331(6019):912-6
  • Gut, 2014, 10.1136/gutjnl-2013-305257
  • Cancer Discov, 2013, 3(6):636-47
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.
  • Cancer Res, 2013, 73(16):5195-205
  • Haematologica, 2011, 96(6):922-6
  • Brit J Cancer, 2011, 104(1):75-82
S7167 SSR128129E SSR128129E is an orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 μM, while not affecting other related RTKs.
S2801 AZD4547 AZD4547 is a novel selective FGFR inhibitor targeting FGFR1/2/3 with IC50 of 0.2 nM/2.5 nM/1.8 nM, weaker activity against FGFR4, VEGFR2(KDR), and little activity observed against IGFR, CDK2, and p38. Phase 2.
  • Cell Physiol Biochem, 2014, 33(3):633-45
  • Celon Pharma Inc., 2013, Paulina Grygielewicz
S1107 Danusertib (PHA-739358) Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2.
  • Cancer Res, 2013, 73(20):6310-22
  • Biochem Pharmacol, 2012, 83(4):452-61
  • J Pharmacol Exp Ther, 2012, 343(3):617-27
S8024 Tyrphostin AG 1296 Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR.
  • Onco Targets Ther, 2014, 7:425-32
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.
  • Haematolog, 2011, 96(6):922-6
  • Expert Opin Investig Drugs, 2014, 10.1517/13543784.2014.885950
  • Oral Oncol, 2012, 48(12):1242-9
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, 2013, 44(3):959-69
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.
S1470 TSU-68 (SU6668, Orantinib) SU6668 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.
  • J Biol Chem, 2014, 10.1074/jbc.M113.547018
  • Mol Cell Proteomics, 2012, 11(9):745-57
  • Angiogenesis, 2012, 15(4):569-80
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. .