WYE-687

WYE-687CAS号: 1062161-90-3分子式: C28H32N8O3分子量: 528.6描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)

产品描述
描述

WYE-687是一种ATP竞争性的,选择性的mTOR抑制剂,IC50为7 nM;抑制mTORC1/pS6K(T389)和mTORC2/P-AKT(S473),但不抑制P-AKT(T308),作用于mTOR比作用于PI3Kα(>100倍)和PI3Kγ(>500倍)选择性高。

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
可溶性/溶解性
DMSO : 25 mg/mL (47.29 mM; ultrasonic and warming and heat to 60°C)
生物活性
靶点
mTOR
In vitro(体外研究)
Immune-complex kinase assay shows mTORC2-specific substrate His6-AKT or the mTORC1 substrate His6-S6K is dose dependently inhibited by WYE-687. WYE-687 globally inhibits mTOR signaling and AKT function in cellular models dose dependently. WYE-678 profoundly inhibits cap-dependent and global protein synthesis in MDA361, human breast cancer cells. WYE-687 shows antiproliferative effects in various cancer cell lines involving G1 cell cycle arrest and selective apoptosis. WYE-687 down-regulate angiogenic factors, VEGF and HIF-1α, in U87MG, MDA361 and LNCap cells.

分子结构图

WYE-687