Futibatinib

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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 : 418.449
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 :

DMSO: 30 mg/mL(71.69 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • FGFR2

    FGFR2, IC50:1.4 nM

  • FGFR3

    FGFR3, IC50:1.6 nM

  • FGFR4

    FGFR4, IC50:3.7 nM

  • FGFR1

    FGFR1, IC50:1.8 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]Goyal L, et al. TAS-120 Overcomes Resistance to ATP-Competitive FGFR Inhibitors in Patients with FGFR2 Fusion-Positive Intrahepatic Cholangiocarcinoma. Cancer Discov. 2019 Aug;9(8):1064-1079.

[2]Kalyukina M, et al. TAS-120 Cancer Target Binding: Defining Reactivity and Revealing the First Fibroblast Growth Factor Receptor 1 (FGFR1) Irreversible Structure. ChemMedChem. 2019 Feb 19;14(4):494-500.

[3]Lamarca A, et al. Molecular targeted therapies: Ready for "prime time" in biliary tract cancer [published online ahead of print, 2020 Mar 12]. J Hepatol. 2020;S0168-8278(20)30165-3.