1144068-46-1

N-[4-[1-(1,4-二氧杂螺[4.5]癸烷-8-基)-4-(8-氧杂-3-氮杂双环[3.2.1]辛烷-3-基)-1H-吡唑并[3,4-d]嘧啶-6-基]苯基]-N'-甲基脲

1144068-46-1

编号ABP000102 化学名称N-[4-[1-(1,4-二氧杂螺[4.5]癸烷-8-基)-4-(8-氧杂-3-氮杂双环[3.2.1]辛烷-3-基)-1H-吡唑并[3,4-d]嘧啶-6-基]苯基]-N'-甲基脲 英文名称 WYE125132/WYE-125132/WYE-132/ MDL: MFCD16038851 分子式C27H33N7O4 分子量519.603 纯度 >98%

化学名称 : N-[4-[1-(1,4-二氧杂螺[4.5]癸烷-8-基)-4-(8-氧杂-3-氮杂双环[3.2.1]辛烷-3-基)-1H-吡唑并[3,4-d]嘧啶-6-基]苯基]-N'-甲基脲

CAS : 1144068-46-1

英文名称: WYE125132/WYE-125132/WYE-132/

英文同义词: WYE-125132

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

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