tcsc0044831 AZ32

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.

IC50 & Target: IC50: <6.2 nM (ATM enzyme), 0.31 μM (ATM, in cell)^[1]

In Vitro: 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].

In Vivo: 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].