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AZD0156

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Chemical Structure| 1821428-35-6 同义名 : -
CAS号 : 1821428-35-6
货号 : A998216
分子式 : C26H31N5O3
纯度 : 99%+
分子量 : 461.556
MDL号 : MFCD30470661
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 18 mg/mL(39 mM)，配合低频超声，并调节pH至3，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
动物实验配方：
生物活性
靶点

  • ATM
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]
实验方案
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
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.