XL147
货号：
18011-50mg 基本售价：
6832.0 元 规格：
50 mg
产品信息
概述| 货号 | 18011-50mg |
| 描述 | The phosphatidylinositol 3-kinase (PI3K) signaling pathway has central roles in cell growth, development, and survival. XL147 is a methylbenzenesulfonamide derivative that reversibly inhibits class I PI3Ks (IC50s = 39, 36, 23, and 383 nM for p110α, δ, γ, and β, respectively).1 It has been shown to abrogate Akt and S6 kinase phosphorylation, reduce cyclin D1 and retinoblastoma protein, and upregulate the CDK inhibitor p27, inhibiting cell proliferation.1 In HER2-overexpressing breast cancer cells, cotreatment with the HER2 inhibitors trastuzumab or lapatinib (Item No. 11493) are reported to sensitize tumor cells to the growth inhibitory effect of XL147.2 This compound has been evaluated in clinical trials in patients with advanced solid tumors.3 |
| 别名 | Pilaralisib;SAR245408; |
性能| 供应商 | Cayman |
| 应用文献 |
1.Akinleye, A.,Avvaru, P.,Furqan, M., et al. Phosphatidylinositol 3-kinase (PI3K) inhibitors as cancer therapeutics. J.Hematol.Oncol. 6(1), (2013).
2.Chakrabarty, A.,Sánchez, V.,Kuba, M.G., et al. Feedback upregulation of HER3 (ErbB3) expression and activity attenuates antitumor effect of PI3K inhibitors. Proceedings of the National Academy of Sciences of the United States of America 109(8), 2718-2723 (2012).
3.Shapiro, G.I.,Rodon, J.,Bedell, C., et al. Phase I safety, pharmacokinetic, and pharmacodynamic study of SAR245408 (XL147), an oral pan-class I PI3K inhibitor, in patients with advanced solid tumors. Clinical Cancer Research 20(1), 233-245 (2014).
|
| 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 | 541 |
| 分子式 | C25H25ClN6O4S |
| CAS号 | 934526-89-3 |
| 稳定性 | ≥ 2 years |
声明| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |
