FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4 . FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4 V550L , FGFR4 V550M and FGFR4 C552S with IC 50 s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC 50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model.
Products | Products > Signaling Pathways > Protein Tyrosine Kinase/RTK | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Signaling Pathways > FGFR
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