FGFR4-IN-8

FGFR4-IN-8 (Compound 7v) is an ATP-competitive inhibitor that covalently and selectively targets both wild-type and gatekeeper mutant forms of FGFR4. It exhibits inhibitory potency with IC50 values of 0.5 nM for FGFR4, 0.25 nM for FGFR4 V550L, 1.6 nM for FGFR4 V550M, and 931 nM for FGFR4 C552S. Additionally, FGFR4-IN-8 shows potent antiproliferative effects on Hep3B hepatocellular carcinoma cells (IC50 of 29 nM) and demonstrates moderate antitumor efficacy in vivo in a Huh-7 xenograft model in nude mice [1].