Name: WYE-125132 (WYE-132)
Price: 434.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    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 [1].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 [1].
    
    [1] 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.
- Properties
  - Alternative Name
    
    1-[4-[1-(1,4-dioxaspiro[4.5]decan-8-yl)-4-(8-oxa-3-azabicyclo[3.2.1]octan-3-yl)pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-3-methylurea
    
    CAS Number
    
    1144068-46-1
    
    Molecular Formula
    
    C27H33N7O4
    
    Molecular Weight
    
    519.61
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥13 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only