Futibatinib

产品说明书

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Chemical Structure| 1448169-71-8 同义名 : TAS-120
CAS号 : 1448169-71-8
货号 : A773884
分子式 : C22H22N6O3
纯度 : 99%+
分子量 : 418.45
MDL号 : MFCD29037352
存储条件:

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
靶点
  • FGFR1

    FGFR1, IC50:1.8 nM

  • FGFR1

    FGFR1, IC50:1.8 nM

  • FGFR3

    FGFR3, IC50:1.6 nM

  • FGFR3

    FGFR3, IC50:1.6 nM

描述 Futibatinib, also referred to as TAS-120, is an orally administered inhibitor of FGFR that is both highly selective and irreversible. It demonstrates IC50 values of 3.9, 1.3, 1.6, and 8.3 nM for FGFRs 1 through 4, respectively. Futibatinib effectively inhibits both the mutant and wild-type forms of FGFR2, with comparable IC50 values (for wild-type FGFR2, the IC50 is 0.9 nM; for V5651, it ranges from 1 to 3 nM; for N550H, it is 3.6 nM; and for E566G, it is 2.4 nM)[1][2][3]. Futibatinib, known by its research name TAS-120, forms a covalent bond with the conserved cysteine residue located in the P-loop within the ATP-binding site of FGFR[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.39mL

0.48mL

0.24mL

11.95mL

2.39mL

1.19mL

23.90mL

4.78mL

2.39mL

参考文献

[1]WO2015008839A1