AZ32
产品说明书
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同义名 : | - |
| CAS号 : | 2288709-96-4 | |
| 货号 : | A667472 | |
| 分子式 : | C20H16N4O | |
| 纯度 : | 99%+ | |
| 分子量 : | 328.37 | |
| MDL号 : | MFCD31715431 | |
| 存储条件： |
Pure form Sealed in dry, room temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Ataxia telangiectasia mutated (ATM) protein is a critical kinase that responds to DNA double-strand breaks (DSB) and reactive oxygen species (ROS) induced by cellular exposures to ionizing radiation (IR) and certain intrinsic stimuli. ATM is an ATP-dependent phosphatidylinositol 3-kinase-related kinase (PIKK) serine/threonine protein kinase related to ATR, DNA-PKcs, mTOR, SMG1, and the nonenzymatic TRRAP within this enzyme family[1]. 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[1]. AZ32 blocked the DNA damage response and radiosensitized GBM cells in vitro[1]. AZ32, with enhanced blood–brain barrier (BBB) penetration, was highly efficient in vivo as radiosensitizer in syngeneic and human, orthotopic mouse glioma model. In vivo, apoptosis was >6-fold higher in tumor relative to healthy brain after exposure to AZ32 and low-dose radiation. 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 are in excess of the cellular IC50 for approximately 22 hours[1]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.05mL 0.61mL 0.30mL |
15.23mL 3.05mL 1.52mL |
30.45mL 6.09mL 3.05mL |
| 参考文献 |
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