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。

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.

AZ32 is an enhanced blood-brain barrier (BBB)-penetrating ATM inhibitor. AZ32 blocks the DNA damage response and radiosensitized GBM cells in vitro[1].

AZ32 has enhanced BBB penetration that 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].

2288709-96-4

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