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  • 5 mg - 284 EUR
  • 25 mg - 1136 EUR
  • 100 mg - 3408 EUR

WYE-125132

WYE-125132 is a highly potent (subnanomolar), ATP-competitive, and specific mTOR kinase inhibitor, with an IC(50) of 0.19 nmol/L for mTOR and >5,000-fold selectivity for mTOR against the PI3Ks. WYE-132 inhibited mTORC1 and mTORC2 in diverse cancer models in vitro and in vivo. Importantly, WYE-132 inhibited the functioning of P-AKT(S473) and AKT without significantly reducing the steady-state level of the PI3K/PDK1 activity biomarker P-AKT(T308). Similar effects are induced by the genetic ablation of mTORC2, which suggests that mTORC plays a prominent and direct role in regulating AKT in cancer cells. Compared to the rapalog temsirolimus/CCI-779, WYE-132 is a significantly more potent inhibitor of cancer cell growth and survival, protein synthesis, cell growth, bioenergetic metabolism, and adaptation to hypoxia.

catalogue number: W091
synonyms: WYE-132
CAS: 1144068-46-1
MW: 519.6 g/mol

References
Cancer Res. 2010 Jan 15;70(2):621-31. PMID: 20068177
J Biol Chem. 2010 May 14;285(20):15380-92. PMID: 20233713