产品描述: AZ32 is an orally bioavailable and blood-brain barrier-penetrating ATM inhibitor with an IC50 of <6.2 nM for ATM enzyme, and an IC50 of 0.31 μM for ATM in cell. |
靶点:
ATM:6.2 nM (IC50);ATM:0.31 μM (IC50, in cell);ATM/ATR |
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 IC50 for approximately 22 hours. |
参考文献:
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. |
溶解性:
Soluble in DMSO |
保存条件:
-20℃ |
配置溶液浓度参考:
|
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 |
50 mM |
0.061 ml |
0.305 ml |
0.609 ml |
|
注意: |
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