| 货号 | 16986-25mg |
| 描述 | BYL719 is a selective inhibitor of phosphoinositide 3-kinase α (PI3Kα) that is equipotent against both wild type and several mutant isoforms (IC50s = 4.0-4.8 nM).1,2 It is less effective against PI3K isoforms β, γ, and δ (IC50s = 1,156, 250, and 290 nM) as well as a range of related kinases.1 BYL719 is effective in vivo, as it dose-dependently inhibits the growth of PI3Kα-dependent xenograft tumors in mice.1 Effectiveness against wild type and mutant PI3Kα-dependent tumors may be augmented by combination therapy with inhibitors of other kinases.3,4,5 Combination therapy may be necessary, as loss of downstream pathway components can confer clinical resistance to BYL719.6 |
| 别名 | Alpelisib;NVP-BYL719; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Fritsch, C.,Huang, A.,Chatenay-Rivauday, C., et al. Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials. Molecular Cancer Therapeutics 13(5), 1117-1129 (2014). 2.Furet, P.,Guagnano, V.,Fairhurst, R.A., et al. Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation. Bioorganic & Medicinal Chemistry Letters 23, 3741-3748 (2013). 3.Young, C.D.,Pfefferle, A.D.,Owens, P., et al. Conditional loss of ErbB3 delays mammary gland hyperplasia induced by mutant PIK3CA without affecting mammary tumor latency, gene expression, or signaling. Cancer Research 73(13), 4075-4085 (2013). 4.Elkabets, M.,Vora, S.,Juric, D., et al. mTORC1 inhibition is required for sensitivity to PI3K p110α inhibitors in PIK3CA-mutant breast cancer. Sci.Transl.Med. 5(196), 1-15 (2013). 5.Gritsman, K.,Yuzugullu, H.,Von, T., et al. Hematopoiesis and RAS-driven myeloid leukemia differentially require PI3K isoform p110α. Journal of Clinical Investigation 124(4), 1794-1809 (2014). 6.Juric, D.,Castel, P.,Griffith, M., et al. Convergent loss of PTEN leads to clinical resistance to a PI(3)Kα inhibitor. Nature 518(7538), 240-244 (2015). | |
| 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 | 441.5 |
| 分子式 | C19H22F3N5O2S |
| CAS号 | 1217486-61-7 |
| 稳定性 | ≥ 2 years |
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