aladdin 阿拉丁 A414140 AZ32 2288709-96-4 99%

中文名：AZ32

英文名：AZ32

纯度：≥99%

货号：A414140

Cas号：2288709-96-4

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

Information

AZ32 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.

Targets

ATM (Cell-free assay) <0.0062 μM

In vitro

AZ32 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 vivo

AZ32, 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 

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