AZ32
| 中文名称 | AZ32 |
|---|---|
| 中文同义词 | N-甲基-4-(6-苯基咪唑[1,2-A]吡嗪-3-)苯甲酰胺;化合物AZ32;N-甲基-4-(6-苯基咪唑并[1,2-A]吡嗪-3-基)苯甲酰胺 |
| 英文名称 | AZ32 |
| 英文同义词 | Benzamide, N-methyl-4-(6-phenylimidazo[1,2-a]pyrazin-3-yl)-;N-Methyl-4-(6-phenylimidazo[1,2-a]pyrazin-3-yl)benzamide;AZ32;Ataxia telangiectasia mutated,ATM and RAD3 related,inhibit,Inhibitor,AZ 32,AZ-32,AZ32,ATM/ATR |
| CAS号 | 2288709-96-4 |
| 分子式 | C20H16N4O |
| 分子量 | 328.37 |
| EINECS号 | |
| 相关类别 | 标准品 |
| Mol文件 | 2288709-96-4.mol |
| 结构式 |  |
AZ32 性质
| 密度 | 1.25±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | 二甲基亚砜：150mg/mL |
| 形态 | 固体 |
| 酸度系数(pKa) | 14.63±0.46(Predicted) |
| 颜色 | 白色至米白色 |
|
ATM 6.2 nM (IC 50 ) |
ATM 0.31 μM (IC 50 , in cell) |
AZ32 is a next-generation blood-brain barrier (BBB)-penetrating ATM inhibitor. AZ32 blocks the DNA damage response and radiosensitized GBM cells in vitro.
AZ32, with enhanced BBB penetration, is highly efficient in vivo as radiosensitizer in syngeneic and human, orthotopic mouse glioma model compared with AZ31. AZ32 is a specific inhibitor of the ATM kinase that possesses good BBB penetration in mouse. Following a single oral dose of AZ32 (200 mg/kg) in mice, the free-brain concentrations of AZ32 are in excess of the cellular IC 50 for approximately 22 hours.