WAY-600 1062159-35-6
WAY600
分子式:C28H30N8O 分子量:494.59
产品描述
WAY-600是有效的,ATP竞争性的,选择性mTORYZ剂,IC50为9 nM;YZmTORC1/P-S6K(T389)和mTORC2/P-AKT(S473),但不YZP-AKT(T308);作用于mTOR比作用于PI3Kα(>100倍)和PI3Kγ(>500倍)选择性高。
靶点
mTOR
IC50
9 nM
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 WAY-600. WAY-600 globally inhibits mTOR signaling and AKT function in cellular models dose dependently. WAY-600 profoundly inhibits cap-dependent and global protein synthesis in MDA361, human breast cancer cells. WAY-600 shows antiproliferative effects in various cancer cell lines involving G1 cell cycle arrest and selective apoptosis. WAY-600 down-regulate angiogenic factors, VEGF and HIF-1α, in U87MG, MDA361 and LNCap cells.
体内研究
溶解性
DMSO 22 mg/mL,水 <1 mg/mL,乙醇 2 mg/mL
稳定性
2年 -20°C粉状,6月-80°C溶于DMSO