A selective inhibitor of FGFR4 (IC50s = 3

BLU-9931 – 5 mg

Brand:
Cayman
CAS:
1538604-68-0
Storage:
-20
UN-No:
Non-Hazardous - /

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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Description

A selective inhibitor of FGFR4 (IC50s = 3, 591, 493, and 150 nM for FGFR4, 1, 2, and 3, respectively); inhibits proliferation of HCC cells (EC50s = 0.02-0.11 µM) and demonstrates antitumor activity in mice bearing HCC xenografts when administered orally at 100 mg/kg

Formal name: N-[2-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-quinazolinyl]amino]-3-methylphenyl]​-2-propenamide

Synonyms: 

Molecular weight: 509.4

CAS: 1538604-68-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|FGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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