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XL147
| 品牌 | 厂商性质 | 产地 | 货期 |
|---|---|---|---|
| 阿拉丁 | 生产商 | 上海 | 现货 |
产品参数
| 货号 | CAS号 | 操作 |
|---|---|---|
| X129499-50mg | 956958-53-5 | 询价 |
| X129499-10mg | 956958-53-5 | 询价 |
产品介绍
- 分子式 C21H16N6O2S2
- 分子量448.52
属性
| 溶解性 | DMSO 3 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
| 存贮条件 | 储存温度-20°C |
描述
| 应用 | An ATP-competetive class I PI3K inhibitor. |
| 产品介绍 | XL147是一种选择性的，可逆的I型PI3K抑制剂，对PI3Kα/δ/γ有抑制作用，IC50分别为39 nM/36 nM/23 nM，对PI3Kβ作用效果稍弱。 |
| 备注 | XL147 is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM, less potent to PI3Kβ. Phase 1/2. |
| 生化机理 | XL-147 derivative 2 is an ATP-competitive inhibitor of class I PI3K isoforms. XL-147 derivative 2 abrogates Akt and S6 phosphorylation in HER2+ cells and also induces the expression and phosphorylation of HER3 and other RTKs. Treatment with the anti-HER2 agents trastuzumab or lapatinib sensitizes HER2+ breast cancer cells to XL-147 derivative 2 in vitro. Treatment with XL-147 derivative 2 inhibits the monolayer growth of all tested cell lines, including BT474, HCC1937 et al. in a dose-dependent manner. XL-147 derivative 2 induces cell death at a concentration of 20 μM by inducing a reduction in cyclin D1 and pRB and increasing in levels of the CDK inhibitor p27KIPI. In HER2-overexpressing cells, inhibition of PI3K is followed by up-regulation of expression and phosphorylation of multiple receptor tyrosine kinases, including HER3. |
| 别名 | XL 147; N-[3-(2,1,3-苯并噻二唑-5-氨基)-2-喹喔啉基]-4-甲基苯磺酰胺;PI3K inhibitor X;N-[3-(2,1,3-Benzothiadiazol-5-ylamino)-2-quinoxalinyl]-4-methylbenzenesulfonamide;XL-147 derivative 2 |
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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途