TAS-120 (Synonyms: TAS-120) |
| رقم الكتالوجGC19156 |
TAS-120 (TAS-120) هو مثبط FGFR متوفر بيولوجيًا عن طريق الفم ، انتقائي للغاية ، ولا رجوع فيه ، مع IC50s من 3.9 و 1.3 و 1.6 و 8.3 نانومتر لـ FGFR 1-4 ، على التوالي. TAS-120 يمنع FGFR2 المتحولة والبرية مع IC50s مماثلة (من النوع البري FGFR2 = 0.9 نانومتر ؛ V5651 = 1-3 نانومتر ؛ N550H = 3.6 نانومتر ؛ E566G = 2.4 نانومتر).
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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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