货号	规格	价格	上海	北京	珠海	重庆	武汉
S83373-1mg买3赠1	98.50%	￥220.00 S83373-1mg ￥220.00 现货（买3赠1）	9 9	-	-	-	-
S83373-5mg买3赠1	98.50%	￥550.00 S83373-5mg ￥550.00 现货（买3赠1）	5 5	-	-	-	-
S83373-10mg买3赠1	98.50%	￥860.00 S83373-10mg ￥860.00 现货（买3赠1）	5 5	-	-	-	-
S83373-50mg	≥98%	￥2840.00 S83373-50mg ￥2840.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM)

靶点：

FGFR1:3.9 nM (IC50);FGFR2:1.3 nM (IC50);FGFR3:1.6 nM (IC50);FGFR4:8.3 nM (IC50);wild-type FGFR2:0.3 nM (IC50);FGFR2 V5651:1-3 nM (IC50);FGFR2 N550H:3.6 nM (IC50);FGFR2 E566G:2.4 nM (IC50);FGFR

体外研究：

Futibatinib (TAS-120) covalently binds to a highly conserved P-loop cysteine residue in the ATP pocket of FGFR

体内研究：

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

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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.39 ml	11.949 ml	23.898 ml
5 mM	0.478 ml	2.39 ml	4.78 ml
10 mM	0.239 ml	1.195 ml	2.39 ml
50 mM	0.048 ml	0.239 ml	0.478 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

FGFR-IN-1