产品描述
| 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 |
| 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 |
