| 货号 | 11587-1mg |
| 描述 | Phosphatidylinositol 3-kinases (PI3K) belong to a family of lipid kinases that is involved in many types of cancer.1 NVP-BKM120 is an orally bioavailable inhibitor of class I PI3K isoforms, potently blocking, in vitro, both p110α (IC50 = 52 nM) and p110β (IC50 = 166 nM).2 It much less effectively inhibits the class III PI3K Vps34 and mammalian target of rapamycin and has no effect on PI4Kβ and several other kinases.2 NVP-BKM120 prevents the growth of assorted cancer cell lines when used at 5 μM and inhibits tumor growth in vivo.3,4 It can be particularly effective against certain types of cancer when combined with other modulators.5,6,7 |
| 别名 | Buparlisib; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Yuan, T.L. and Cantley, L.C. PI3K pathway alterations in cancer: Variations on a theme. Oncogene 27(41), 5497-5510 (2008). 2.Maira, S.M.,Pecchi, S.,Huang, A., et al. Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor. Molecular Cancer Therapeutics 11(2), 317-328 (2012). 3.Pei, Y.,Moore, C.E.,Wang, J., et al. An animal model of MYC-driven medulloblastoma. Cancer Cell. 21(2), 155-167 (2012). 4.Koul, D.,Fu, J.,Shen, R., et al. Antitumor activity of NVP-BKM120--a selective pan class I PI3 kinase inhibitor showed differential forms of cell death based on p53 status of glioma cells. Clinical Cancer Research 18(1), 184-195 (2012). 5.Aziz, S.A.,Jilaveanu, L.B.,Zito, C., et al. Vertical targeting of the phosphatidylinositol-3 kinase pathway as a strategy for treating melanoma. Clinical Cancer Research 16(24), 6029-6039 (2010). 6.Buonamici, S.,Williams, J.,Morrissey, M., et al. Interfering with resistance to smoothened antagonists by inhibition of the PI3K pathway in medulloblastoma. Sci.Transl.Med. 2(51), (2010). 7.Park, E.,Park, J.,Han, S.W., et al. NVP-BKM120, a novel PI3K inhibitor, shows synergism with a STAT3 inhibitor in human gastric cancer cells harboring KRAS mutations. International Journal of Oncology 40(4), 1259-1266 (2012). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 410.4 |
| 分子式 | C18H21F3N6O2 |
| CAS号 | 944396-07-0 |
| 稳定性 | ≥ 2 years |
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