BLU-9931
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Technical Data
Description
BLU-9931 is a potent and irreversible small-molecule inhibitor of FGFR4. BLU-9931 is exquisitely selective for FGFR4 versus other FGFR family members and all other kinases, as shown FGFR4 activity (IC50 = 3 nmol/L), but FGFR1 (IC50 = 591 nmol/L), FGFR2 (IC50 = 493 nmol/L), and FGFR3 (IC50 = 150 nmol/L) activity. BLU-9931 shows remarkable antitumor activity in mice bearing an HCC tumor xenograft that overexpresses FGF19 due to amplification as well as a liver tumor xenograft that overexpresses FGF19 mRNA but lacks FGF19 amplification.
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