AZD0156
Based on 18 publication(s) in Google Scholar
AZD0156 is a potent, selective and orally active ATM inhibitor with an IC50 of 0.58 nM. AZD0156 inhibits the ATM-mediated signaling, prevents DNA damage checkpoint activation, disrupts DNA damage repair, and induces tumor cell apoptosis.
For research use only. We do not sell to patients.
- Purity: 99.83%
- CAS No.: 1821428-35-6
- Formula: C26H31N5O3
- Molecular Weight:461.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) AZD0156
More- Cancer Discov. 2020 Nov;10(11):1742-1757. [Abstract]
- Sci Signal. 2023 Aug;16(796):eade8744. [Abstract]
- Mol Cancer Ther. 2026 Jul 15:10.1158/1535-7163.MCT-26-0182.
- EMBO Rep. 2024 Mar;25(3):1469-1489. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- Cancers (Basel). 2021 Aug 20;13(16):4200. [Abstract]
- iScience. 2026 Feb 19;29(3).
- PLoS One. 2022 Sep 23;17(9):e0274735. [Abstract]
- Portland State University. 2026.
- bioRxiv. 2026 Jun 2.
- bioRxiv. 2026 May 1:2026.04.28.717272. [Abstract]
- bioRxiv. 2025 Oct 15.
- bioRxiv. 2025 Oct 9:2025.10.08.680157. [Abstract]
- Biomed Pharmacother. 2025 Aug:189:118273. [Abstract]
- bioRxiv. 2025 May 15:2025.05.13.652823. [Abstract]
- Patent. US20250161243A1.
- Research Square Preprint. 2023 Jun 9.
- bioRxiv. 2023 Mar 21:2023.03.17.533211. [Abstract]
Customer Validation & Images
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Gel Electrophoresis
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
Biological Activity
Description
IC50 & Target
[1]|
ATM |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.46 nM
Compound: AZD0156
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Inhibition of colony formation in human HCT-116 cells preincubated for 1 hr followed by exposure to 2 Gy gamma irradiation and measured after 1 week by crystal violet staining based chemiluminescence assay
Inhibition of colony formation in human HCT-116 cells preincubated for 1 hr followed by exposure to 2 Gy gamma irradiation and measured after 1 week by crystal violet staining based chemiluminescence assay
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[PMID: 37438997] |
| MCF7 | IC50 |
0.6 μM
Compound: 6; AZD-0156
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Antiproliferative activity against human MCF7 cells measured after 2 days by SRB assay
Antiproliferative activity against human MCF7 cells measured after 2 days by SRB assay
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[PMID: 35231830] |
| SW480 | IC50 |
1.1 μM
Compound: 6; AZD-0156
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Antiproliferative activity against human SW480 cells measured after 3 days by SRB assay
Antiproliferative activity against human SW480 cells measured after 3 days by SRB assay
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[PMID: 35231830] |
In Vitro
AZD0156 inhibits the kinase activity of ATM and ATM-mediated signaling, prevents DNA damage checkpoint activation, and disrupts DNA damage repair, inducs tumor cell apoptosis, and leads to cell death in ATM-overexpressing tumor cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1821428-35-6
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Appearance Solid
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Molecular Weight 461.56
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Formula C26H31N5O3
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Color White to off-white
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SMILES
O=C(N1C2CCOCC2)N(C)C3=C1C4=CC(C5=CC=C(OCCCN(C)C)N=C5)=CC=C4N=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (18)
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Journal Impact Factor
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Most Recent
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Cancer Discov
PRMT5 Inhibition Modulates E2F1 Methylation and Gene-Regulatory Networks Leading to Therapeutic Efficacy in JAK2V617F-Mutant MPN. [Abstract]2020 Nov;10(11):1742-1757. PMID: 32669286 -
Sci Signal
Multiple cancers escape from multiple MAPK pathway inhibitors and use DNA replication stress signaling to tolerate aberrant cell cycles. [Abstract]2023 Aug;16(796):eade8744. PMID: 37527351 -
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EMBO Rep
Tumor acidosis-induced DNA damage response and tetraploidy enhance sensitivity to ATM and ATR inhibitors. [Abstract]2024 Mar;25(3):1469-1489. PMID: 38366255
AZD0156 purchased from MedChemExpress. Usage Cited in: EMBO Rep. 2024 Mar;25(3):1469-1489. [Abstract]
Cell viability assays in HCT116 and HT-29 cancer cells cultured at pH 7.4 or 6.5, and treated with the indicated doses of ATMi AZD0156 (0.01-10 μM) for 72 h.
AZD0156 purchased from MedChemExpress. Usage Cited in: EMBO Rep. 2024 Mar;25(3):1469-1489. [Abstract]
(C, D) Effects of 10 µM ATMi AZD0156, 10 µM 5-FU or the combination of both drugs on the growth of colorectal cancer patient-derived tumor organoids. Representative pictures of organoids at day 7 post-treatment are presented (C) together with quantification (D). Scale bars = 500 µm.
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J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Cancers (Basel)
Novel Insights into the Molecular Regulation of Ribonucleotide Reductase in Adrenocortical Carcinoma Treatment. [Abstract]2021 Aug 20;13(16):4200. PMID: 34439352 -
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PLoS One
2022 Sep 23;17(9):e0274735. PMID: 36149903
AZD0156 purchased from MedChemExpress. Usage Cited in: PLoS One. 2022 Sep 23;17(9):e0274735. [Abstract]
Results of inducing white turbidity with galactose as in C (upper panel) and a subsequent 2–4 days in galactose medium containing AZD0156 dissolved in DMSO to final concentrations of 2.5, 5, 10, 20, and 40 μM (lower panel).
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bioRxiv
2026 May 1:2026.04.28.717272. PMID: 42094395 -
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bioRxiv
2025 Oct 9:2025.10.08.680157. PMID: 41279244
AZD0156 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Oct 9:2025.10.08.680157. [Abstract]
pICLPt was replicated in egg extract supplemented with [α-32P]dCTP and the ATM inhibitor AZD0156, as indicated. Replication intermediates were resolved on a native agarose gel. As with KU-55933 treatment, AZD0156 (100 μM; 30-240 min) treatment resulted in stabilization of reversed fork intermediates and suppressed formation of okadaic acid-induced putative fork cleavage products.
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Biomed Pharmacother
Synergistic suppression of cholangiocarcinoma cells via DNA damage response and cell cycle arrest by dual targeting PARP and ATM in DNA damage repair pathway. [Abstract]2025 Aug:189:118273. PMID: 40527032
AZD0156 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2025 Aug:189:118273. [Abstract]
Dose-response curves obtained using the MTS assay in niraparib-sensitive CCA cell lines after treatment with AZD0156 at concentrations of 5-15 μM for 72 h.
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bioRxiv
2025 May 15:2025.05.13.652823. PMID: 40462982 -
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bioRxiv
Multiple cancer types rapidly escape from multiple MAPK inhibitors to generate mutagenesis-prone subpopulations. [Abstract]2023 Mar 21:2023.03.17.533211. PMID: 36993538
Solvent & Solubility
In Vitro:
DMSO : 20 mg/mL (43.33 mM; ultrasonic and adjust pH to 3 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
DMSO : 20 mg/mL (43.33 mM; ultrasonic and adjust pH to 3 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 0.83 mg/mL (1.80 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 0.83 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 0.83 mg/mL (1.80 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 0.83 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Cell Assay[1]
HT29 cells are seeded into 384 well assay plates at a density of 6000 cells/well in 40 μL EMEM medium containing 1% L glutamine and 10% FBS and allowed to adhere overnight. The following morning compound of Formula (I) in 100% DMSO is added to assay plates by acoustic dispensing. After lh incubation at 37°C and 5% C02, 40 nL of 3 mM 4NQO in 100% DMSO is added to all wells by acoustic dispensing, except minimum control wells which are left untreated with 4NQO to generate a null response control. Plates are returned to the incubator for a further lh. Then cells are fixed by adding 20 μL of 3.7% formaldehyde in PBS solution and incubating for 20 mins at r.t.. Then 20 μL of 0.1% Triton XI 00 in PBS is added and incubated for 10 minutes at r.t., to permeabalise cells. Then the plates are washed once with 50 μL/well PBS, using a Biotek EL405 plate washer.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / DMSO | 1 mM | 2.1666 mL | 10.8328 mL | 21.6657 mL | 54.1641 mL |
| 5 mM | 0.4333 mL | 2.1666 mL | 4.3331 mL | 10.8328 mL | |
| 10 mM | 0.2167 mL | 1.0833 mL | 2.1666 mL | 5.4164 mL | |
| 15 mM | 0.1444 mL | 0.7222 mL | 1.4444 mL | 3.6109 mL | |
| 20 mM | 0.1083 mL | 0.5416 mL | 1.0833 mL | 2.7082 mL | |
| 25 mM | 0.0867 mL | 0.4333 mL | 0.8666 mL | 2.1666 mL | |
| 30 mM | 0.0722 mL | 0.3611 mL | 0.7222 mL | 1.8055 mL | |
| 40 mM | 0.0542 mL | 0.2708 mL | 0.5416 mL | 1.3541 mL |
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