BLU-9931

BLU-9931

CAT N°: 18405
Price:

From 74.00 62.90

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).{30600} 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).{30600} 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.{30600}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • N-[2-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-quinazolinyl]amino]-3-methylphenyl]?-2-propenamide
  • Correlated keywords
    • BLU9931 irreversible FGFR4 FGFR fibroblast growth factor receptor HCC hepatocellular carcinoma FGFR4FGF19 FGF-19
  • Product Overview:
    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).{30600} 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).{30600} 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.{30600}

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