AZ32 是一种口服生物利用度和血脑屏障穿透性 ATM 抑制剂，对 ATM 酶的 IC50<6.2 nM，对细胞内 ATM 的 IC50 为 0.31 μM。
货号:ajcx11586
CAS:2288709-96-4
分子式:C20H16N4O
分子量：328.37
溶解度:DMSO : ≥ 150 mg/mL (456.80 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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 uM for ATM 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[1].

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[1].

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.