| 货号 | 21185-10mg |
| 描述 | NVP-BEZ235 is a potent dual inhibitor of phosphatidylinositol 3-kinase (PI3K) and mTOR that is well tolerated, displays disease stasis when administered orally, and enhances the efficacy of other anticancer agents when used in in vivo combination studies.1,2 It inhibits PI3K isoforms and mutants with low nanomolar IC50 values, leading to growth arrest in the G1phase.1,3 Through its effects on PI3K, NVP-BEZ235 inhibits VEGF-induced angiogenesis.4 By directly blocking cell growth and indirectly inhibiting angiogenesis, it has potential in both solid tumors and in metastatic melanoma therapy.5,6 |
| 别名 | Dactolisib; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Maira, S.M.,Stauffer, F.,Brueggen, J., et al. Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Molecular Cancer Therapeutics 7(7), 1851-1863 (2008). 2.Zitzmann, K.,von Rüden, J.,Brand, S., et al. Compensatory activation of Akt in response to mTOR and Raf inhibitors - A rationale for dual-targeted therapy approaches in neuroendocrine tumor disease. Cancer Letters 295, 100-109 (2010). 3.Serra, V.,Markman, B.,Scaltriti, M., et al. NVP-BEZ235, a dual PI3K/mTOR inhibitor, prevents PI3K signaling and inhibits the growth of cancer cells with activating PI3K mutations. Cancer Research 68(19), 8022-8030 (2008). 4.Schnell, C.R.,Stauffer, F.,Allegrini, P.R., et al. Effects of the dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235 on the tumor vasculature: Implications for clinical imaging. Cancer Research 68(16), 6598-6607 (2008). 5.Marone, R.,Erhart, D.,Mertz, A.C., et al. Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors. Molecular Cancer Research 7(4), 601-613 (2009). 6.Brachmann, S.M.,Hofmann, I.,Schnell, C., et al. Specific apoptosis induction by the dual PI3K/mTOR inhibitor NVP-BEZ235 in HER2 amplified and PIK3CA mutant breast cancer cells. Proceedings of the National Academy of Sciences of the United States of America 106(52), 22299-22304 (2009). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 506 |
| 分子式 | C30H23N5O • HCl |
| 稳定性 | ≥ 2 years |
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