WYE-687  1062161-90-3

WYE687
分子式：C28H32N8O3  分子量：528.61
 
產品描述
WYE-687是ATP競爭性的，選擇性mTOR抑制劑，IC50為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)選擇性高。
靶點
mTOR
         
IC50
7 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 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.
體內研究
 
溶解性
DMSO 0.5 mg/mL，水 <1 mg/mL，乙醇 <1 mg/mL
穩定性
2年 -20°C粉狀，6月-80°C溶于DMSO