产品描述
| 熔点 | 248-251 °C |
| 溶解性 | Soluble in DMSO (12 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), ethanol (<1 mg/ml at 25 °C), and 30% PEG400/0.5% Tween80/5% propylene glycol (30 mg/ml at 25 °C). |
| 存贮条件 | 储存温度-20°C |
| 应用 | A potent class I PI3K inhibitor |
| 产品介绍 | SAR245409 (XL765)是作用于mTOR/PI3K的双重抑制剂，对p110γ作用最强，IC50为9 nM；也可抑制DNA-PK和mTOR。 |
| 备注 | SAR245409 (XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2. |
| 生化机理 | XL-147 derivative 1 is active against class I PI3K (IC50 = 39, 113, 9 and 43 nM for p110α, β, γ and δ, respectively). XL765 also inhibits DNA-PK (IC50 = 150 nM) and mTOR (IC50 = 157 nM) but not XL-147 which shows IC50 values of > 15 μM. [1] XL765 treatment results in decreased cell viability in 13 PDA cell lines in a dose-dependent manner. XL-147 derivative 1, a dual-target PI3K/mTOR inhibitor, inhibits cell growth and apoptosis in many more cell lines and at lower concentrations as compared to the PI3K-selective inhibitors XL147 and PIK90. |
| 别名 | N-[4-[[[3-[(3,5-二甲氧基苯基)氨基]-2-喹喔啉基]氨基]磺酰基]苯基]-3-甲氧基-4-甲基苯甲酰胺;XL-147 derivative 1;N-[4-({3-[(3,5-dimethoxyphenyl)amino]quinoxalin-2-yl}sulfamoyl)phenyl]-3-methoxy-4-methylbenzamide;PI3K-IN-1 |
