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Futibatinib C화학적 특성, 용도, 생산
용도
Futibatinib is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with potential antineoplastic activity. Futibatinib selectively and irreversibly binds to and inhibits FGFR, which may result in the inhibition of both the FGFR-mediated signal transduction pathway and tumor cell proliferation, and increased cell death in FGFR-overexpressing tumor cells. FGFR is a receptor tyrosine kinase essential to tumor cell proliferation, differentiation and survival and its expression is upregulated in many tumor cell types.
in vitro
Futibatinib (TAS-120) covalently binds to a highly conserved P-loop cysteine residue in the ATP pocket of FGFR.
in vivo
Futibatinib (TAS-120) (3, 30, 100 mg/kg/day, p.o.) exerts an anti-tumor
effect in mice. Futibatinib (TAS-120) shows anti-tumor effect by
administering at moderate intervals, such as intermittent administration
of every other day dosing and 2 times/week, and reducing the sustained
elevation and weight suppression blood phosphorus level, and take a
antitumor effective as daily administration.
