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FGFR-IN-1 is an inhibitor of FGF receptor 4 (FGFR4; IC50 = 1.3 nM).1 It is selective for FGFR4 over FGFR1 and a panel of 36 kinases (IC50s = >10 µM for all). It inhibits proliferation of Hep3B and Huh7 hepatic cancer cells with IC50 values of 1.1 and 2.5 nM, respectively. FGFR-IN-1 reduces tumor growth by 62.7 and 70.8% in a Huh7 mouse xenograft model when administered at doses of 30 and 100 mg/kg per day, respectively.
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