• FGFR2
  • FGFR3
  • FGFR4

FGFR4 Selective Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S8548 Roblitinib (FGF401) Roblitinib (FGF401) is an FGFR4-selective inhibitor with an IC50 of 1.1 nM. It binds in a reversible covalent manner to the FGFR4 kinase domain and shows at least 1,000 fold selectivity against of panel of 65 kinases in biochemical assays. Selective FGFR4, IC50: 1.1 nM
S8675 H3B-6527 H3B-6527 is a highly selective covalent FGFR4 inhibitor with an IC50 value of <1.2 nM and at least 250-fold selectivity over FGFR1-3 (IC50 values of 320, 1,290 and 1,060 nM respectively). Selective FGFR4, IC50: <1.2 nM
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. Selective FGFR4, IC50: 3 nM
S8503 Fisogatinib (BLU-554) Fisogatinib (BLU-554) is a potent, highly-selective, oral FGFR4 inhibitor with an IC50 value of 5 nM. The IC50s for FGFR1-3 is 624-2203 nM. Selective FGFR4, IC50: 5 nM
S6539 ASP5878 ASP5878 is a novel FGFR-selective inhibitor with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L for recombinant FGFR1, 2, 3, and 4, respectively. Pan FGFR4, IC50: 3.5 nM
S8848 Futibatinib (TAS-120) Futibatinib (TAS-120) is an irreversible fibroblast growth factor receptor (FGFR) inhibitor which inhibits all 4 subtypes of FGFR with enzyme IC50 values of 1.8 nM, 1.4 nM, 1.6 nM and 3.7 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. Pan FGFR4, IC50: 3.7 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. Pan FGFR4, IC50: 6 nM
S8578 PRN1371 PRN1371 is an irreversible covalent FGFR1-4 kinase inhibitor, with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, 2, 3, 4 and CSF1R, respectively. Pan FGFR4, IC50: 19.3 nM
S0088 Pemigatinib (INCB054828) Pemigatinib (INCB054828, Pemazyre) is an orally active and selective inhibitor of FGFR with IC50 of 0.4 nM, 0.5 nM, 1.2 nM and 30 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma. Pan FGFR4, IC50: 30 nM
S8609 Derazantinib(ARQ-087) Derazantinib(ARQ-087) is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3, showing lower potency for FGFR4 (IC50=34 nM). It also inhibits RET, DDR2, PDGFRβ, VEGFR and KIT. Pan FGFR4, IC50: 34 nM
S8882 ODM-203 ODM-203 is a selective inhibitor of FGFR and VEGFR with ic50s of 11 nM,16 nM,6 nM, 35 nM,26 nM,9 nM,5 nM for recombinant FGFR1, FGFR2, FGFR3,FGFR4, VEGFR1, VEGFR2 and VEGFR3, respectively. Pan FGFR4, IC50: 35 nM
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. Pan FGFR4, IC50: 45.3 nM
S2183 Infigratinib (BGJ398) Infigratinib (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. Pan FGFR4, IC50: 60 nM
S7665 Zoligratinib (Debio-1347) Zoligratinib (Debio-1347, CH5183284, FF284) 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. Pan FGFR4, IC50: 290 nM
S1010 Nintedanib (BIBF 1120) Nintedanib (BIBF 1120, Intedanib, Vargatef, Ofev) 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. Pan FGFR4, IC50: 610 nM