An inhibitor of ATM kinase (IC50s = 0.04 and 0.57 nM in enzyme and cell-based assays

AZD 0156 – 10 mg

Brand:
Cayman
CAS:
1821428-35-6
Storage:
-20
UN-No:
Non-Hazardous - /

AZD 0156 is an inhibitor of the ataxia-telangiectasia mutated (ATM) kinase (IC50s = 0.04 and 0.57 nM in enzyme and cell-based assays, respectively).{48018} It is selective for ATM over other PI3K-related kinase (PIKK) family kinases including DNA-PK, mTOR, PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ (IC50s = 0.14, 0.20, 0.32, 1.8, 1.1, and 0.27 μM, respectively, in enzyme assays). AZD 0156 (20 mg/kg) enhances the antitumor activity of irinotecan (Item No. 14180) in an SW620 colon cancer mouse xenograft model and olaparib (Item No. 10621) in an HBCx-10 breast cancer patient-derived xenograft (PDX) mouse model when administered at a dose of 5 mg/kg, leading to tumor regression in both models.  

 

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Description

An inhibitor of ATM kinase (IC50s = 0.04 and 0.57 nM in enzyme and cell-based assays, respectively); selective for ATM over other PIKK family kinases including DNA-PK, mTOR, PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ (IC50s = 0.14, 0.20, 0.32, 1.8, 1.1, and 0.27 μM, respectively, in enzyme assays); enhances the antitumor activity of irinotecan in an SW620 colon cancer mouse xenograft model at 20 mg/kg and olaparib in an HBCx-10 breast cancer PDX mouse model at 5 mg/kg, leading to tumor regression in both models

Formal name: 8-[6-[3-(dimethylamino)propoxy]-3-pyridinyl]-1,3-dihydro-3-methyl-1-(tetrahydro-2H-pyran-4-yl)-2H-imidazo[4,5-c]quinolin-2-one

Synonyms: 

Molecular weight: 461.6

CAS: 1821428-35-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|ATM||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|ATM Signaling||Research Area|Cancer|DNA Damage and Repair

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