| 货号 | 15320-1mg |
| 描述 | p70 Ribosomal S6 kinase (p70S6K) is a serine/threonine kinase that is activated by insulin and growth factors through PI3K and mTORC1 signaling pathways. LY2584702 is a selective, cell-permeable p70S6K inhibitor (IC50 = 4 nM). It blocks phosphorylation of p70S6K in primary rat hepatocytes without affecting the phosphorylation of other signaling kinases, including GSK-3β and ERK1/2.1 LY2584702 inhibits phosphorylation of p70S6K in HCT116 colon cancer cells (IC50 = 0.1-0.24 μM in vitro) and demonstrates significant antitumor efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models.2 It also reverses the effects of mTORC1 hyperactivation on triglyceride metabolism in human hepatoma cells.3 LY2584702, alone or in combination with the mTOR inhibitor everolimus (Item No. 11597), has been evaluated in clinical trials against solid tumors.2,4 |
| 别名 | LYS6K2; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Li, S.,Brown, M.S. and Goldstein, J.L. Bifurcation of insulin signaling pathway in rat liver: mTORC1 required for stimulation of lipogenesis, but not inhibition of gluconeogenesis. Proceedings of the National Academy of Sciences of the United States of America 107(8), 3441-3446 (2010). 2.Tolcher, A.,Goldman, J.,Patnaik, A., et al. A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumours. European Journal of Cancer 50(5), 867-875 (2014). 3.Roberts, J.L.,He, B.,Erickson, A., et al. Improvement of mTORC1-driven overproduction of apoB-containing triacylglyceride-rich lipoproteins by short-chain fatty acids, 4-phenylbutyric acid and (R)-α-lipoic acid, in human hepatocellular carcinoma cells. Biochim.Biophys.Acta. 1861(3), 166-176 (2016). 4.Hollebecque, A.,Houédé, N.,Cohen, E.E., et al. A phase Ib trial of LY2584702 tosylate, a p70 S6 inhibitor, in combination with erlotinib or everolimus in patients with solid tumours. European Journal of Cancer 50(5), 876-884 (2014). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 617.6 |
| 分子式 | C21H19F4N7 • C7H8O3S |
| CAS号 | 1082949-68-5 |
| 稳定性 | ≥ 2 years |
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