FGFR

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FGFR Inhibitors (20)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
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 in cell-free assays, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. Phase 2.
  • Cancer Cell, 2015, 27(1):97-108
  • Hepatology, 2014, 59(4):1427-34
  • Chem Biol, 2014, 21(10):1310-7
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
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 in cell-free assays, weaker activity against FGFR4, VEGFR2(KDR), and little activity observed against IGFR, CDK2, and p38. Phase 2/3.
  • Nat Commun, 2015, 6:7002
  • Oncogene, 2016, 10.1038/onc.2016.216
  • J Neurosci, , 36(16):4534-48
S7167 SSR128129E SSR128129E is an orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 μM, while not affecting other related RTKs.
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.
S7714 FIIN-2 FIIN-2 is an irreversible, pan-FGFR inhibitor with IC50 of 3.09 nM, 4.3 nM, 27 nM and 45.3 nM for FGFR1/2/3/4, respectively.
S7667 SU5402 SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.
  • Oncogene, 2016, 10.1038/onc.2016.244
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
  • Cancer Discov, 2016, 6(7):727-39
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
  • Am J Respir Crit Care Med, 2015, 192(4):455-67
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 Inv Drugs, 2014, 23(4):469-87
Cat.No. Product Name Information Product Use Citation Customer Product Validation
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 in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2.
  • Cancer Res, 2014, 74(20):5878-90
  • Cancer Res, 2013, 73(20):6310-22
  • Biochem Pharmacol, 2012, 83(4):452-61
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 USA, 2014, 111(44):E4706-15
  • Mol Cell Proteomics, 2012, 11(9):745-57
  • Angiogenesis, 2012, 15(4):569-80
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.
  • Genome Biol, 2014, 15(8):428
  • Eur J Cancer, 2016, 61:20-8
  • Int J Oncol, 2014, 44(3):959-69
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.
  • Cancer Lett, 2016, 380(1):163-173
  • Expert Opin Inv Drugs, 2014, 23(4):469-87
  • Br J Cancer, 2011, 104(1):75-82
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. .
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.
  • Int J Oncol, 2014, 44(3):959-69
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
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.
  • Genome Biol, 2014, 15(8):428
S7665 CH5183284 (Debio-1347) CH5183284 is a selective and orally available FGFR inhibitor with IC50 of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. Phase 1.
S7819 BLU9931 BLU9931 is a potent, selective, and irreversible FGFR4 inhibitor with IC50 of 3 nM, about 297-, 184-, and 50-fold selectivity over FGFR1/2/3, respectively.
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All FGFR Products

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S2183 BGJ398 (NVP-BGJ398) <1 mg/mL 1 mg/mL <1 mg/mL
S1264 PD173074 <1 mg/mL 100 mg/mL 100 mg/mL
S2801 AZD4547 <1 mg/mL 92 mg/mL <1 mg/mL
S7167 SSR128129E 1 mg/mL 69 mg/mL <1 mg/mL
S7057 LY2874455 <1 mg/mL 88 mg/mL 57 mg/mL
S7714 FIIN-2 <1 mg/mL 69 mg/mL <1 mg/mL
S7667 SU5402 <1 mg/mL 59 mg/mL <1 mg/mL
S1490 Ponatinib (AP24534) <1 mg/mL 30 mg/mL <1 mg/mL
S1010 Nintedanib (BIBF 1120) <1 mg/mL 6 mg/mL 3 mg/mL
S1018 Dovitinib (TKI-258, CHIR-258) <1 mg/mL 30 mg/mL <1 mg/mL
S1107 Danusertib (PHA-739358) <1 mg/mL 95 mg/mL <1 mg/mL
S1470 TSU-68 (SU6668, Orantinib) <1 mg/mL 62 mg/mL <1 mg/mL
S1084 Brivanib (BMS-540215) <1 mg/mL 74 mg/mL 3 mg/mL
S2769 Dovitinib (TKI-258) Dilactic Acid 70 mg/mL 90 mg/mL <1 mg/mL
S2774 MK-2461 <1 mg/mL 99 mg/mL <1 mg/mL
S1138 Brivanib Alaninate (BMS-582664) <1 mg/mL 88 mg/mL 88 mg/mL
S8024 Tyrphostin AG 1296 <1 mg/mL 6 mg/mL <1 mg/mL
S7765 Dovitinib (TKI258) Lactate 66 mg/mL 100 mg/mL 1 mg/mL
S7665 CH5183284 (Debio-1347) <1 mg/mL 71 mg/mL 1 mg/mL
S7819 BLU9931 <1 mg/mL 4 mg/mL <1 mg/mL
Tags: FGFR inhibition | FGFR signaling | FGFR pathway | FGFR phosphorylation | FGFR activation | FGFR inhibitors clinical trials | FGFR inhibitor review
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