Wortmannin-Rapamycin Conjugate
货号：
13671-5mg 基本售价：
13888.0 元 规格：
5 mg
产品信息
概述| 货号 | 13671-5mg |
| 描述 | Phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) act synergistically in promoting cancer. Wortmannin is a potent inhibitor of PI3K enzymes, while rapamycin blocks mTOR Complex 1 TORC1.1,2 Wortmannin-rapamycin conjugate consists of analogs of 17-hydroxy wortmannin and rapamycin conjugated via a prodrug linker.3 Hydrolysis of the prodrug linker in vivo releases the inhibitors. The wortmannin-rapamycin conjugate inhibits the growth of HT-29 colon tumors and A498 renal tumors in mice better than rapamycin alone.3 Also, the conjugate, when given in combination with the VEGF-blocker bevacizumab, produces substantial regression of larger A498 tumors. Finally, the wortmannin-rapamycin conjugate is tolerated better than an equivalent mixture of the inhibitors.3 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Fruman, D.A.,Meyers, R.E. and Cantley, L.C. Phosphoinositide kinases. Annual Reviews of Biochemistry 67, 481-507 (2008).
2.Carracedo, A. and Pandolfi, P.P. The PTEN-PI3K pathway: Of feedbacks and cross-talks. Oncogene 27, 5527-5541 (2008).
3.Ayral-Kaloustian, S.,Gu, J.,Lucas, J., et al. Hybrid inhibitors of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR): Design, synthesis, and superior antitumor activity of novel wortmannin-rapamycin conjugates. Journal of Medicinal Chemistry 53(1), 452-459 (2010).
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| 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 | 1598.9 |
| 分子式 | C88H131N3O23 |
| CAS号 | 1067892-47-0 |
| 稳定性 | ≥ 2 years |
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