WYE-125132
货号:
18372-500ug 基本售价:
546.0 元 规格:
500 ug
产品信息
概述货号 | 18372-500ug |
描述 | The mammalian target of rapamycin (mTOR) is a serine-threonine kinase that is central to two protein complexes, mTORC1 and mTORC2. These complexes are differentially regulated (e.g., only mTORC1 is sensitive to rapamycin (Item No. 13346)) and regulate different pathways. WYE-125132 is an ATP-competitive inhibitor of mTOR (IC50 = 0.19 nM) that inhibits signaling through both mTORC1 and mTORC2.1 It is selective for mTOR over phosphatidylinositol 3-kinase isoforms.1 WYE-125132 is effective against mTORC1 and mTORC2 in diverse cancer models, both in vitroandin vivo.1 Oral administration of WYE-125132 alone blocks mTOR signaling and prevents tumor growth in breast, lung, renal, and glioma cancer xenografts in mice, while combination therapy with the VEGF-inhibitor bevacizumab causes complete regression of A498 renal carcinoma tumors.1 In addition to its applications in cancer, WYE-125132 has been used to delineate novel aspects of mTOR signaling.2 |
别名 | WYE-132; |
性能供应商 | Cayman |
应用文献 |
1.Yu, K.,Shi, C.,Toral-Barza, L., et al. Beyond rapalog therapy: preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2. Cancer Research 70(2), 621-631 (2010). 2.Shor, B.,Wu, J.,Shakey, Q., et al. Requirement of the mTOR kinase for the regulation of Maf1 phosphorylation and control of RNA polymerase III-dependent transcription in cancer cells. The Journal of Biological Chemisty 285(20), 15380-15392 (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 | 519.6 |
分子式 | C27H33N7O4 |
CAS号 | 1144068-46-1 |
稳定性 | ≥ 2 years |
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