WYE-125132 (WYE-132)1144068-46-1

WYE125132 (WYE-132)
分子式：C27H33N7O4   分子量：519.6
 
產(chǎn)品描述
WYE-125132 是高度有效的，ATP競爭性的，mTOR抑制劑，IC50為0.19 nM;作用于mTOR比作用于PI3Ks或PI3K相關激酶hSMG1和ATR選擇性高。
靶點
mTOR
         
IC50
0.19 nM
         
體外研究
WYE-125132 potently and ATP-competitively inhibits recombinant mTOR kinase with IC50 of 0.19 nM and also shows the high selectivity over various PI3Ks and a panel of 230 protein kinases.In vitro, WYE-125132 exhibits a significant anti-proliferative activity against a panel of tumor cell lines with IC50 ranging from 2 nM (LNCap) to 380 nM (HTC116). Besides, WYE-125132 also causes cell cycle progression, induction of apoptosis, and inhibition of protein synthesis and cell size.WYE-125132 results in a significant reduction in the synthesis of pre-tRNALeu by 72%, 80%, and 53% in actively proliferating cells of MG63, MDA361, and HEK293, respectively by inhibiting mTORC1. Moreover, WYE-125132 is also found to induce the dephosphorylation of Maf1 (negative regulator of Pol III transcription) and its accumulation in the nucleus.
體內(nèi)研究
WYE-125132 (5 mg/kg p.o.) produces significant antitumor activity and causes dose-dependent tumor growth delay in the PI3K/mTOR- and HER2-hyperactive MDA361 tumor model. In addition, WYE-125132 also shows potent antitumor efficacy in the PTEN-null glioma U87MG, non-small cell lung cancer H1975 and A549 models.
溶解性
DMSO 104 mg/mL，水 <1 mg/mL，乙醇 <1 mg/mL
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO
特征
WYE-125132 is a highly potent, ATP-competitive, and specific mTOR kinase inhibitor.