WYE-354-d3
花椒毒酚
WYE-354-d3
花椒毒酚
WYE-354-d3
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产品编号： CWR950002
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CAS号： 1794791-66-4
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相关CAS号：1062169-56-5（未标记）
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分子式：C11H6O4
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分子量：202.16
英文别名：
9-Hydroxy-7H-furo[3,2-g][1]benzopyran-7-one; 6,7-Dihydroxy-5-benzofuranacrylic Acid δ-Lactone; 3-(6,7-Dihydroxy-5-benzofuranyl)-2-propenoic Acid δ-Lactone; 8-Hydroxypsoralen; NSC 401269;
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 labelled 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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