| 货号 | 11597-5mg |
| 描述 | The mammalian target of rapamycin (mTOR) is a serine/threonine kinase that, as part of two distinct complexes (mTORC1 and mTORC2), plays pivotal roles in intracellular signaling.1,2,3 Everolimus is a hydroxyethyl ether rapamycin (Item No. 13346) derivative that inhibits mTOR signaling through both mTORC1 and mTORC2 when added to cells at 20 nM.4,5 It is orally available and shows improved pharmacokinetics and pharmacodynamics over rapamycin.5 Through its inhibition of mTOR, everolimus inhibits cell proliferation, metabolism, and angiogenesis in certain types of cancer.6,7 It also acts as an immunosuppressive agent in the context of organ transplantation.5,8 |
| 别名 | Afinitor®;Certican;NVP-RAD001;RAD001; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Petroulakis, E.,Mamane, Y.,Le Bacquer, O., et al. mTOR signaling: implications for cancer and anticancer therapy. British Journal of Cancer 94, 195-199 (2006). 2.Dann, S.G.,Selvaraj, A. and Thomas, G. mTOR complex1-S6K1 signaling: At the crossroads of obesity, diabetes and cancer. Trends in Molecular Medicine N/A, 1-8 (2007). 3.Tao, Z.,Barker, J.,Shi, S.D.H., et al. Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes. Biochem. 49(39), 8488-8498 (2010). 4.Zeng, Z.,Sarbassov, D.D.,Samudio, I.J., et al. Rapamycin derivatives reduce mTORC2 signaling and inhibit AKT activation in AML. Blood 109(8), 3509-3512 (2007). 5.Lebwohl, D.,Anak, Ö.,Sahmoud, T., et al. Development of everolimus, a novel oral mTOR inhibitor, across a spectrum of diseases. Ann. N.Y. Acad. Sci. 1291, 14-32 (2013). 6.Yunokawa, M.,Koizumi, F.,Kitamura, Y., et al. Efficacy of everolimus, a novel mTOR inhibitor, against basal-like triple-negative breast cancer cells. Cancer Sci. 103(9), 1665-1671 (2012). 7.Gurk-Turner, C.,Manitpisitkul, W. and Cooper, M. A comprehensive review of everolimus clinical reports: A new mammalian target of rapamycin inhibitor. Transplantation 94(7), 659-668 (2012). | |
| 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 | 958.2 |
| 分子式 | C53H83NO14 |
| CAS号 | 159351-69-6 |
| 稳定性 | ≥ 2 years |
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