WYE-354
mTOR 抑制剂
WYE-354
mTOR 抑制剂
WYE-354
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产品编号： CWR950000
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CAS号： 1062169-56-5
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分子式：C24H29N7O5
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分子量：495.53
英文别名：
4-[6-[4-[(Methoxycarbonyl)amino]phenyl]-4-(4-morpholinyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinecarboxylic Acid Methyl Ester
SMILES：
O=C1C2=C3C(=CC=C2)C=CC=C3C(=O)N1CCCSC1N(C2C=CC(OC)=CC=2)C(C2C=CN=CC=2)=NN=1
参考文献：
Yu, K. et al.: Cancer Res., 69, 6232 (2009); Zask, A. et al.: J. Med. Chem., 52, 5-13 (2009); Dormind-Meuwly, A. et al.: Biochem. Biophys. Res. Comm., 407, 714 (2011);
A pyrazolopyrimidines derivative that is a potent and ATP-competitive mTOR inhibitor with much reduced activity against PI 3-Kα or PI 3-Kγ. WYE-354 is equally potent against mTORC1 and mTORC2 activities in HEK293 immune complex kinase assays using S6K and Akt as the respective substrate (IC50 <200 nM; [ATP] = 100 µM) and effectively blocks cellular phosphorylation of S6K on T389 and Akt on S473 both in cultures and in a murine xenograft model, resulting in a significant suppression of PC3MM2-derived tumor growth (by 86% on day 7; 50 mg/kg, i.p twice per day) in vivo.
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