产品说明书
AZD1390
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同义名 : | - |
| CAS号 : | 2089288-03-7 | |
| 货号 : | A775616 | |
| 分子式 : | C27H32FN5O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 477.574 | |
| MDL号 : | MFCD31619275 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 4 mg/mL(8.38 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The ataxia-telangiectasia mutated (ATM) protein kinase is a master regulator of the DNA damage response (DDR), and it coordinates checkpoint activation, DNA repair, and metabolic changes in eukaryotic cells in response to DNA double-strand breaks and oxidative stress[1]. AZD1390 is a potent, highly selective, orally bioavailable, brain-penetrant ATM inhibitor with an IC50 of 0.78 nM in cell[2]. AZD1390 blocks ATM-dependent DDR pathway activity and combines with radiation to induce G2 cell cycle phase accumulation, micronuclei, and apoptosis. AZD1390 radiosensitizes glioma and lung cancer cell lines, with p53 mutant glioma cells generally being more radiosensitized than wild type[2]. In in vivo syngeneic and patient-derived glioma as well as orthotopic lung-brain metastatic models, AZD1390 dosed in combination with daily fractions of ionizing radiation (IR) (whole-brain or stereotactic radiotherapy) significantly induced tumor regressions and increased animal survival compared to IR treatment alone[2]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT03215381 | Healthy Volunteer Male Subject... 展开 >>s 收起 << | Phase 1 | Completed | - | Sweden ... 展开 >> Research Site Stockholm, Sweden, 171 76 收起 << |
| NCT03423628 | Recurrent Glioblastoma Multifo... 展开 >>rme Primary Glioblastoma Multiforme Brain Neoplasms, Malignant Leptomeningeal Disease (LMD) 收起 << | Phase 1 | Recruiting | April 5, 2021 | United States, Massachusetts ... 展开 >> Research Site Recruiting Boston, Massachusetts, United States, 02215 United States, New York Research Site Recruiting New York, New York, United States, 10065 United States, Pennsylvania Research Site Recruiting Pittsburgh, Pennsylvania, United States, 15232 United States, Virginia Research Site Recruiting Richmond, Virginia, United States, 23294 United Kingdom Research Site Recruiting Cambridge, United Kingdom, CB2 0QQ Research Site Recruiting Glasgow, United Kingdom, G12 0YN Research Site Recruiting Leeds, United Kingdom 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.09mL 0.42mL 0.21mL |
10.47mL 2.09mL 1.05mL |
20.94mL 4.19mL 2.09mL |
| 参考文献 |
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