TAE-226

TAE-226CAS号: 761437-28-9分子式: C23H25ClN6O3分子量: 468.94描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述

TAE226 (NVP-TAE226) is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2, ~10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met.

纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
TAE226, TAE-226,TAE 226,NVPTAE226
外观
Powder
可溶性/溶解性
DMSO 94 mg/mL (200.45 mM)
生物活性
靶点
PYK2 ,FAK ,Insulin Receptor ,IGF-1R ,c-Met
In vitro(体外研究)
NVP-TAE226 ( NVP-TAE226 (5 μM) inhibits phosphorylation of FAK in the human neuroblastoma cell line SK-N-AS. NVP-TAE226 ( NVP-TAE226 (0.1 μM-10 μM) inhibits tube formation of HMEC1 cells.
In vivo(体内研究)
NVP-TAE226 (75 mg/kg) significantly increases the survival rate of mice bearing intracranial glioma xenografts. NVP-TAE226 (100 mg/kg, oral) exerts significant decrease in microvessel density in a human colon cancer model in SCID mice. NVP-TAE226 (100 mg/kg, oral) efficiently inhibits MIA PaCa-2 human pancreatic tumor growth without body weight loss in vivo model. NVP-TAE226 inhibits 4T1 murine breast tumor growth and metastasis to the lung in a dose-dependent manner in vivo model, associated with inhibition of FAK autophosphorylation at Y397 and Akt phosphorylation at Serine473.

分子结构图

TAE-226