WAY-600  1062159-35-6 

WAY600
分子式：C28H30N8O  分子量：494.59
 
產(chǎn)品描述
WAY-600是有效的，ATP競(jìng)爭(zhēng)性的，選擇性mTOR抑制劑，IC50為9 nM;抑制mTORC1/P-S6K(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)選擇性高。
靶點(diǎn)
mTOR
         
IC50
9 nM
         
體外研究
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.
體內(nèi)研究
 
溶解性
DMSO 22 mg/mL，水 <1 mg/mL，乙醇 2 mg/mL
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO