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Catalog#: C-1085 Targets: FGFR4 Synonym: BLU9931; BLU-9931; BLU 9931 Chemical Name/IUPAC: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
Product Name: BLU-9931 Chemical Formula: C26H22Cl2N4O3 Molecular Weight: 509.38 CAS#: 1538604-68-0 Appearance: Solid powder Purity: > 99% by HPLC Solubility: Soluble in DMSO Storage: Room temperature for months, or -20ºC for 3 years
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.