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 |
XL147,PI3K抑制剂
XL147 (订货以英文为准)
编号:X129499
CAS号:956958-53-5
分子式:C21H16N6O2S2
分子量:448.52
产品名称 | XL147 |
中文名称 | XL147,PI3K抑制剂 |
CAS号 | 956958-53-5 |
分子式(M.F.) | C21H16N6O2S2 |
分子量(M.W.) | 448.52 |
储存条件 | -20°C储存 |
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