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Futibatinib

CAS No. : 1448169-71-8

MCE 国际站：Futibatinib

产品活性：Futibatinib (TAS-120) 是一种口服生物利用度高、选择性强、不可逆的 FGFR 抑制剂，对 FGFR 1-4 的 4 个亚型的 IC₅₀ 分别为 3.9、1.3、1.6 和 8.3 nM。Futibatinib 抑制突变型和野生型 FGFR2，且 IC₅₀ 相似 (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM)。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：FGFR

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.

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