TAS-120 (Synonyms: TAS-120) |
| カタログ番号GC19156 |
TAS-120 (TAS-120) は、経口で生物学的に利用可能な、選択性の高い不可逆的な FGFR 阻害剤であり、FGFR 1 ～ 4 の IC50 はそれぞれ 3.9、1.3、1.6、および 8.3 nM です。 TAS-120 は、類似の IC50 で変異体および野生型 FGFR2 を阻害します (野生型 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.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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.
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *