1144068-46-1

溶解度:DMSO

储存条件:-20°C for 2 years 

生物活性

WYE-125132 (WYE-132), a highly potent,
ATP-competitive, and specific mTOR kinase inhibitor (IC50: 0.19 ± 0.07 nmol/L; >5,000-fold selective versus
PI3Ks). WYE-132 inhibited mTORC1 and mTORC2 in diverse cancer models in vitro and in vivo. Importantly,
consistent with genetic ablation of mTORC2, WYE-132 targeted P-AKT(S473) and AKT function without significantly
reducing the steady-state level of the PI3K/PDK1 activity biomarker P-AKT(T308), highlighting a
prominent and direct regulation of AKT by mTORC2 in cancer cells. Compared with the rapalog temsirolimus/
CCI-779, WYE-132 elicited a substantially stronger inhibition of cancer cell growth and survival, protein
synthesis, cell size, bioenergetic metabolism, and adaptation to hypoxia

参考文献

Beyond Rapalog Therapy: Preclinical Pharmacology and
Antitumor Activity of WYE-125132, an ATP-Competitive