Cayman BLU-9931

Fibroblast growth factor receptor 4 (FGFR4) is the receptor for fibroblast growth factor 19 (FGF19), which is a tightly controlled hormone that regulates bile acid synthesis and hepatocyte proliferation in the normal liver. Aberrant signaling through the FGFR4/FGF19 signaling complex has been implicated in hepatocellular carcinoma (HCC). BLU-9931 is a small molecule inhibitor of FGFR4 (IC₅₀ = 3 nM) that is selective for FGFR4 over other FGFR family members (IC₅₀s = 591, 493, and 150 nM for FGFR1, 2, and 3, respectively) and an extensive panel of additional kinases (selectivity score for BLU-9931 at 3 µM is 0.005). It inhibits proliferation of HCC cell lines with an activated FGFR4 signaling pathway (EC₅₀s = 0.02-0.11 µM) and demonstrates antitumor activity when administered orally at 100 mg/kg to mice bearing HCC xenografts that overexpresses FGF19 due to amplification or to mice bearing liver tumor xenografts that overexpresses FGF19 mRNA but lack FGF19 amplification.

WARNING This product is not for human or veterinary use.