BLU9931

BLU9931 is an **orally bioavailable, selective, and irreversible small-molecule inhibitor** of human **fibroblast growth factor receptor 4 (FGFR4)**, developed primarily as a potential targeted therapy for cancers where aberrant FGF19/FGFR4 signaling is implicated, such as hepatocellular carcinoma (HCC), pancreatic cancer, and certain renal cancers. BLU9931 irreversibly binds the cysteine residue at position 552 in the FGFR4 active site, blocking autophosphorylation and downstream kinase activity, leading to inhibition of tumor cell growth, induction of apoptosis, and cell cycle arrest. BLU9931 is highly selective for FGFR4 over other FGFR paralogs and kinases. Its development has primarily been preclinical, and it has been discontinued before entering clinical trials, probably due to pharmacokinetic limitations such as rapid hepatic metabolism[1][2][3][4][5][6][7][9].

Other names

1538604-68-0N-[2-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl]amino]-3-methylphenyl]prop-2-enamide