An ATM kinase inhibitor
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AZD 0156

Item No. 25648

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
CAS Number
1821428-35-6
Molecular Formula
C26H31N5O3
Formula Weight
461.6
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
210, 273 nm
SMILES
CN(C)CCCOC(C=C1)=NC=C1C2=CC3=C(C=C2)N=CC4=C3N(C5CCOCC5)C(N4C)=O
InChi Code
InChI=1S/C26H31N5O3/c1-29(2)11-4-12-34-24-8-6-19(16-28-24)18-5-7-22-21(15-18)25-23(17-27-22)30(3)26(32)31(25)20-9-13-33-14-10-20/h5-8,15-17,20H,4,9-14H2,1-3H3
InChi Key
AOTRIQLYUAFVSC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $129

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    10 mg

    $205

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    25 mg

    $382

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    50 mg

    $636

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    Product Description

    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).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Pike, K.G., Barlaam, B., Cadogan, E., 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. 61(9), 3823-3841 (2018).