WYE-125132 (WYE-132) is highly potent, ATP-competitive, and specific inhibitor of mTOR kinase with IC50 value of 0.19±0.07nmol/L, ＞5000-fold selective versus PI3Ks .
WYE-125132 (WYE-132) has been reported to mTORC1-dependent phosphorylation of S6K (T389) and mTORC2-dependent phos-phorylation of AKT (S473) in immune-complex assay. In addition, in insulin-like growth factor-I(IGF-I)–induced Rat1, the PIK3CA mutant MDA361, or PTEN-null U87MG cells, WYE-125132 (WYE-132) has also been revealed to dose-dependently inhibit P-S6K(T389) and P-AKT(S473) with EC50 in low nanomolar range. Apart from these, WYE-125132 (WYE-132) has shown a potent anti-proliferative agent against MDA361, PC3MM2, U87MG, A549, and HCT116 cell lines. Moreover, WYE-125132 (WYE-132) has noted a stronger inhibition of protein synthesis and cell size in MDA361 and HEK293 cell lines .
 Yu K1, Shi C, Toral-Barza L, Lucas J, Shor B, Kim JE, Zhang WG, Mahoney R, Gaydos C, Tardio L, Kim SK, Conant R, Curran K, Kaplan J, Verheijen J, Ayral-Kaloustian S, Mansour TS, Abraham RT, Zask A, Gibbons JJ. Beyond rapalog therapy: preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2. Cancer Res. 2010 Jan 15;70(2):621-31. doi: 10.1158/0008-5472.CAN-09-2340. Epub 2010 Jan 12.
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥13mg/mL in DMSO|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
|Description||WYE-125132 (WYE-132) is a highly potent, ATP-competitive inhibitor of mTOR with an IC50 value of 0.19 nM.|