TAS-120 (Synonyms: TAS-120) |
| Catalog No.GC19156 |
TAS-120(TAS-120)은 FGFR 1-4에 대해 각각 3.9, 1.3, 1.6 및 8.3 nM의 IC50을 갖는 경구 생체 이용률, 고도로 선택적이고 비가역적인 FGFR 억제제입니다. TAS-120은 유사한 IC50으로 돌연변이체 및 야생형 FGFR2를 억제합니다(야생형 FGFR2=0.9nM; V5651=1-3nM; N550H=3.6nM; E566G=2.4nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1448169-71-8
Sample solution is provided at 25 µL, 10mM.
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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].
References:
[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.
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