中文名 | AZ32 |
英文名 | AZ32 |
别名 | 化合物AZ32 N-甲基-4-(6-苯基咪唑[1,2-A]吡嗪-3-)苯甲酰胺 |
英文别名 | AZ32 N-Methyl-4-(6-phenylimidazo[1,2-a]pyrazin-3-yl)benzamide Benzamide, N-methyl-4-(6-phenylimidazo[1,2-a]pyrazin-3-yl)- |
CAS | 2288709-96-4 |
化学式 | C20H16N4O |
分子量 | 328.37 |
溶解度 | DMSO : ≥ 150 mg/mL (456.80 mM) |
存储条件 | -20℃ |
靶点 | ATM |
体外研究 | AZ32 is a next-generation blood-brain barrier (BBB)-penetrating ATM inhibitor. AZ32 blocks the DNA damage response and radiosensitized GBM cells in vitro. |
体内研究 | 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. |
参考资料 展开查看 | 1. Karlin J, et al. Orally Bioavailable and Blood-Brain Barrier-Penetrating ATM Inhibitor (AZ32) Radiosensitizes Intracranial Gliomas in Mice. Mol Cancer Ther. 2018 Aug;17(8):1637-1647. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.045 ml | 15.227 ml | 30.453 ml |
5 mM | 0.609 ml | 3.045 ml | 6.091 ml |
10 mM | 0.305 ml | 1.523 ml | 3.045 ml |
5 mM | 0.061 ml | 0.305 ml | 0.609 ml |
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