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| 25mg |
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Purity: ≥98%
AZD0156 is a novel, orally bioactive, potent and selective inhibitor of ATM (ataxia telangiectasia mutated) kinase with an IC50 of 0.58 nM and with potential chemo-/radio-sensitizing and antineoplastic activities. In addition to blocking DNA damage checkpoint activation and disrupting DNA damage repair, AZD0156 inhibits the kinase activity of ATM and ATM-mediated signaling. This results in tumor cell apoptosis and ultimately leads to cell death in ATM-overexpressing tumor cells. Based on its sub-nanomolar potency in cell-based assays for ATM inhibition, AZD0156 was found to be the first oral ATM inhibitor of its kind. Furthermore, AZD0156 exhibited selectivities over 1000 times greater than those of other PIKK family enzymes.
| Targets |
ATM
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
In tumor cells that overexpress ATM, AZD0156 causes cell death by inhibiting the kinase activity of ATM and ATM-mediated signaling, blocking DNA damage checkpoint activation, disrupting DNA damage repair, and inducing tumor cell apoptosis.
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| Cell Assay |
HT29 cells are cultivated at a density of 6000 cells/well in 384-well assay plates using 40 μL EMEM medium supplemented with 10% FBS and 1% L glutamine, and left to adhere for the entire night. Assay plates are filled with the Formula (I) compound in 100% DMSO the next morning using an acoustic dispensing method. All wells receive 40 nL of 3 mM 4NQO in 100% DMSO by acoustic dispensing following a 1-hour incubation at 37°C and 5% CO2, with the exception of the minimum control wells, which are left untreated with 4NQO in order to produce a null response control. The plates are put back in the incubator to continue lh. Subsequently, 20 μL of 3.7% formaldehyde in PBS solution is added to the cells, and they are incubated for 20 minutes at room temperature to fix them. After that, 20 μL of 0.1% Triton XI 00 in PBS is added, and the cells are incubated for 10 minutes at room temperature to allow for permeabilization. Subsequently, the plates are cleaned once using a Biotek EL405 plate washer and 50 μL/well PBS.
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| References |
| Molecular Formula |
C26H31N5O3
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| Molecular Weight |
461.56
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| Exact Mass |
461.24
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| Elemental Analysis |
C, 67.66; H, 6.77; N, 15.17; O, 10.40
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| CAS # |
1821428-35-6
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| Related CAS # |
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| Appearance |
White to off-white solid powder
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| SMILES |
CN1C2=CN=C3C=CC(=CC3=C2N(C1=O)C4CCOCC4)C5=CN=C(C=C5)OCCCN(C)C
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| InChi Key |
AOTRIQLYUAFVSC-UHFFFAOYSA-N
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| 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
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| Chemical Name |
8-[6-[3-(dimethylamino)propoxy]pyridin-3-yl]-3-methyl-1-(oxan-4-yl)imidazo[4,5-c]quinolin-2-one
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 0.83 mg/mL (1.80 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 0.83 mg/mL (1.80 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 0.83 mg/mL (1.80 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1666 mL | 10.8328 mL | 21.6657 mL | |
| 5 mM | 0.4333 mL | 2.1666 mL | 4.3331 mL | |
| 10 mM | 0.2167 mL | 1.0833 mL | 2.1666 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02588105 | Completed | Drug: AZD0156 Drug: Olaparib |
Advanced Solid Tumours | AstraZeneca | November 10, 2015 | Phase 1 |
Products are for research use only; We do not sell to patients
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