CAS:1352608-82-2EW 7197

Synonyms: Vactosertib;TEW-7197

EW-7197 is a selective inhibitor of TGF-β receptor ALK4 and ALK5 with IC50s of 13 nM and 11 nM.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

技术信息

CAS号

1352608-82-2

储存条件

分子式

C22H18FN7

运输

蓝冰

分子量

399.42

别名

Vactosertib;TEW-7197

溶解度

动物实验配方

5%DMSO+40%PEG400+5% tween80+H2O

5 mg/mL

clear

生物活性

描述EW-7197 is a potent and selective ALK5/ALK4 with IC50 values of 13nM/17nM. It inhibited cellular ALK5 activity with IC50 values of 16.5nM and 12.1nM measured by a luciferase assay in HaCaT (3TP-luc) stable cells and 4T1 (3TP-luc) stable cells, respectively. EW-7197 dose-dependently reduced TGFβ1-induced Smad3 phosphorylation at concentration>30nM in 4T1 cells post 30min, and blocked Smad2/3 nuclear translocation at 1μM. Also it inhibited TGFβ1-induced 4T1 cell migration and invasion as well as inhibited EMT in breast cancer cells. Administration of EW-7197 at doses of 0.625, 1.25, 2.5 and 5mg/kg dose-dependently prolonged the life span of BALB/c 4T1 mice via inhibition of EMT. It inhibited metastasis and enhanced the activity of cytotoxic T lymphocytes in 4T1 orthotopic–grafted mice at dose of 20mg/kg.
作用机制The [1,2,4]triazolo[1,5-a]pyridin-6-yl moiety of EW-7197 occupies the pocket for adenine ring of ATP and commonly forms a hydrogen bonding with NH of His283 in the backbone of hinge region of ALK5.^[1]

动物研究

剂量

Mice: 2.5 mg/kg^[3] (p.o.); 40 mg/kg^[2] (i.p.) Rat: 20 mg/kg^[4] (p.o.)

给药途径

p.o., i.p.

动物药代数据