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Description: BLU9931 (BLU-9931; BLU 9931) is an irreversible and selective FGFR4 inhibitor with potential anticancer activity. It inhibits FGFR4 with an IC50 of 3 nM in a cell-free assay. BLU9931 shows high selectivity for inhibiting FGFR4 over other FGFR family kinases such as FGFR1/2/3 (297-, 184-, and 50-fold selectivity, respectively). BLU9931 exhibits remarkable antitumor activity in mice model bearing an HCC tumor xenograft that overexpresses FGF19 and a liver tumor xenograft model that overexpresses FGF19 mRNA.
References: Cancer Discov. 2015 Apr; 5(4):424-37.
Chemical Name: N-(2-((6-(2, 6-dichloro-3, 5-dimethoxyphenyl)quinazolin-2-yl)amino)-3-methylphenyl)acrylamide
SMILES Code: C=CC(NC1=CC=CC(C)=C1NC2=NC=C3C=C(C4=C(Cl)C(OC)=CC(OC)=C4Cl)C=CC3=N2)=O
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