产品名称

Vactosertib (TEW-7197)

一般描述

Vactosertib is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor.

别 称

2-fluoro-N-[[5-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-1H-imidazol-2-yl]methyl]aniline

纯 度

≥98.0%(HPLC)

CAS NO.

1352608-82-2

分子式

C²²H¹⁸FN⁷

分子量

399.42

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

固体

溶解性(25℃)

DMSO

≥50mg/mL

乙醇

≥40mg/mL

水

Insoluble

l  生物学信息

生物活性/药理作用

Vactosertib is an orally bioavailable inhibitor of the serine/threonine kinase, transforming growth factor (TGF)-beta receptor type 1 (TGFBR1), also known as activin receptor-like kinase 5 (ALK5), with potential antineoplastic activity. Upon oral administration, vactosertib inhibits the activity of TGFBR1 and prevents TGF-beta/TGFBR1-mediated signaling. This suppresses tumor growth in TGFBR1-overexpressing tumor cells. TGFBR1, which is overexpressed in a variety of tumor cell types, plays a key role in tumor cell proliferation. of TGF-beta promotes tumor cell proliferation, enhances the migration of tumor cells and suppresses the response of the host immune system to tumor cells.

Vactosertib is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively.

l  存储

存储温度

-20℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov