| 产品描述： | ATM 选择性抑制剂 | 活化剂;ATM Selective Inhibitors | Activators;AZ32是ATM kinase的特异性抑制剂，在小鼠中具有良好的血脑屏障通透性，对ATM酶的IC5值小于0.0062 μM。它具有充分的选择性和高细胞透性。;InformationAZ32 is a specific inhibitor of theATM kinasethat possesses good BBB penetration in mouse with an IC50 value of <0.0062 μM for ATM enzyme. It shows adequate selectivity over ATR and also has high cell permeability.TargetsATM (Cell-free assay) <0.0062 μMIn vitroAZ32 blocks the DNA damage response (DDR) and radiosensitized GBM cells in vitro. AZ32 shows moderate potency against ATM in cell (IC50 = 0.31 μM) and adequate selectivity over ATR, while also having high cell permeability.In vivoAZ32, with enhanced blood-brain barrier (BBB) penetration, was highly efficient in vivo as radiosensitizer in syngeneic and human, orthotopic mouse glioma model compared with AZ31. AZ32 is the first ATMi with oral bioavailability shown to radiosensitize glioma and improve survival in orthotopic mouse models. Following a single oral dose of AZ32 (200 mg/kg) in mice, the free brain concentrations of AZ32 was in excess of the cellular IC50 for approximately 22 hr. AZ32 has enhanced BBB penetration at 8.7-fold and improved brain coverage over AZ31 but with reduced ATM selectivity.Cell Research(from reference)Cell lines：U1242 cells Concentrations：3 μM Incubation Time：48 h |
| 体内研究： |
与 AZ31 相比，AZ32 具有增强的 BBB 穿透性，在同源和人类原位小鼠神经胶质瘤模型中作为放射增敏剂在体内是高效的。AZ32 是 ATM 激酶的特异性抑制剂，在小鼠体内具有良好的 BBB 穿透能力。小鼠单次口服 AZ32 (200 mg/kg) 后，AZ32 的游离脑浓度超过细胞 IC50 约 22 小时。 |
| 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. |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 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： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京