| 货号 | 17379-1mg |
| 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. OSI-027 is an inhibitor of the catalytic site of mTOR and, as a result, inhibits both mTORC1 and mTORC2 (IC50s = 22 and 65 nM, respectively).1,2 It is selective for mTOR over phosphatidylinositol 3-kinase isoforms and DNA protein kinase.2 OSI-027 prohibits proliferation, induces autophagy, and potentiates apoptosis in BCR-ABL transformed cells and other cancer cells at 10 µM.1,3,4 OSI-027 is effective in vivo, blocking the phosphorylation of targets of mTORC1 and mTORC2 and suppressing tumor growth in several different human xenograft models.2,5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Carayol, N.,Vakana, E.,Sassano, A., et al. Critial roles for mTORC2- and rapamycin-insensitive mTORC1-complexes in growth and survival of BCR-ABL-expressing leukemic cells. Proceedings of the National Academy of Sciences of the United States of America 107(28), 12469-12474 (2010). 2.Falcon, B.L.,Barr, S.,Gokhale, P.C., et al. Reduced VEGF production, angiogenesis, and vascular regrowth contribute to the antitumor properties of dual mTORC1/mTORC2 inhibitors. Cancer Research 71(5), 1573-1583 (2011). 3.Gupta, M.,Hendrickson, A.E.W.,Yun, S.S., et al. Dual mTORC1/mTORC2 inhibition diminishes Akt activation and induces puma-dependent apoptosis in lymphoid malignancies. Blood 119(2), 476-487 (2012). 4.Vakana, E.,Sassano, A. and Platanias, L.C. Induction of autophagy by dual mTORC1-mTORC2 inhibition in BCR-ABL-expressing leukemic cells. Autophagy 6(7), 966-967 (2010). 5.Bhagwat, S.V.,Gokhale, P.C.,Crew, A.P., et al. Preclinical characterization of OSI-027, a potent and selective inhibitor of mTORC1 and mTORC2: Distinct from rapamycin. Molecular Cancer Therapeutics 10(8), 1394-1406 (2011). | |
| 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 | 406.4 |
| 分子式 | C21H22N6O3 |
| CAS号 | 936890-98-1 |
| 稳定性 | ≥ 2 years |
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