AZD0156
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货号：A998216
AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities.
AZD0156 化学结构
AZD0156 3D分子结构
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会员价
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AZD0156 纯度/质量文件 产品仅供科研
货号：A998216
标准纯度：
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产品说明书
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AZD0156 质控信息
AZD0156 生物活性
靶点
描述
AZD0156 is a clinical candidate and selective ATM inhibitor with IC50 value of 5.7nM (>10,000 fold selectivity to ATM than ATR), possessing highly solubility and excellent preclinical pharmacokinetic properties. Co-administration of AZD0156 orally could potentiated the efficacy of both irinotecan (50mg/kg) in an SW620 xenograft model at dose of 20mg/kg, QD, for 2-4 weeks and olaparib (50mg/kg) in a HBCx-10 patient derived tumor xenograft model at dose of 5mg/kg, QD, for 1-3 weeks.
作用机制
AZD0156 interacts with the ATP binding site of ATM.[1]
AZD0156 动物研究
Dose
Mice: 5 mg/kg[2] [3]
Administration
p.o.
Pharmacokinetics
Animal
Rats[3]
Dogs[3]
F
0.57
0.54
CL
15.5 ml/min/kg
33.3 ml/min/kg
T1/2
4.4 h
7.6 h
Vss
4.3 L/kg
17.6 L/kg
AZD0156 参考文献
[1] Lan P, Romero FA, et al. Hit-to-Lead Optimization and Discovery of 5-((5-([1,1'-Biphenyl]-4-yl)-6-chloro-1H-benzo[d]imidazol-2-yl)oxy)-2-methylbenzoic Acid (MK-3903): A Novel Class of Benzimidazole-Based Activators of AMP-Activated Protein Kinase. J Med Chem. 2017 Nov 9;60(21):9040-9052.
[2] Jones GN, Rooney C, et al. pRAD50: a novel and clinically applicable pharmacodynamic biomarker of both ATM and ATR inhibition identified using mass spectrometry and immunohistochemistry. Br J Cancer. 2018 Nov;119(10):1233-1243.
[3] Pike KG, Barlaam B, et al. The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2 H-pyran-4-yl)-1,3-dihydro-2 H-imidazo[4,5- c]quinolin-2-one). J Med Chem. 2018 May 10;61(9):3823-3841.
AZD0156 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
2.17mL
0.43mL
0.22mL
10.83mL
2.17mL
1.08mL
21.67mL
4.33mL
2.17mL
AZD0156 技术信息
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