2288709-96-4

AZ32 is a next-generation blood-brain barrier (BBB)-penetrating ATM inhibitor. AZ32 blocks the DNA damage response and radiosensitized GBM cells in vitro.

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.