AZ32
规格
| Cas Number | 2288709-96-4 |
| 规格或纯度 | ≥99% |
| 纯度 | ≥99% |
| 包装 | 100mg 或 50mg 或 10mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 66 mg/mL (200.99 mM); Ethanol: 7 mg/mL (21.31 mM); Water: Insoluble; |
| 简短描述 | ATM 选择性抑制剂 | 活化剂 |
| 英文简短描述 | ATM Selective Inhibitors | Activators |
| 过滤标签 | ATM/ATR,Cell Cycle/DNA Damage,PI3K/Akt/mTOR |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | AZ32 是 ATM 激酶的特异性抑制剂，在小鼠体内具有良好的 BBB 穿透性，对 ATM 酶的 IC50 值小于 0.0062 μM。它对 ATR 具有充分的选择性，同时还具有较高的细胞渗透性。 |
| 英文描述 |
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 |