TAS-120

An orally bioavailable, irreversible inhibitor of FGFRs

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数量
1mg

￥637.00

510.00

- +
5mg

￥1625.00

1300.00

- +
10mg

￥2400.00

1920.00

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25mg

￥4525.00

3620.00

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50mg

￥7012.00

5610.00

- +

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Background

Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor. Futibatinib (TAS-120) covalently binds to a highly conserved P-loop cysteine residue in the ATP pocket of FGFR. Futibatinib (TAS-120) exhibits potency at low nanomolar concentrations and high specificity against wild-type FGFR1/2/3/4 as well as against some FGFR2 kinase domain mutations[1][2].

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[1].

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.

Protocol

Animal experiment:

It is transplanted to the right chest of the anti-tumor effect human gastric cancer strain (OCUM-2MD3) the old 6-week-old male nude rats with intermittent administration schedule in Test Example 7 rat. Measuring the major axis of tumor (mm) and minor axis (mm) after tumor implantation, the tumor volume: After calculating the (tumor volume TV), allocates the mouse average TV each group to be equal in each group, the the days that are conducted grouped the (n=5) is the day 0. Futibatinib (TAS-120) 3 mg/kg/day, 30 mg/kg/day, is prepared so as to 100 mg/kg/day, 3 mg/kg/day is daily administered orally, 30 mg/kg/day is administered orally every other day, 100 mg/kg/day is performed oral administration of 2 time/week from day 1, provided with the evaluation period of 14 days, the final valuation date it is day 15.

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.