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> AZD0156 [1821428-35-6]

AZD0156 [1821428-35-6]

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Référence HY-100016-5mg

Conditionnement : 5mg

Marque : MedChemExpress


Description

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[1].

IC50 & Target[1]

ATM

 

Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
0.46 nM
Compound: AZD0156
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
[PMID: 37438997]
MCF7 IC50
0.6 μM
Compound: 6; AZD-0156
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
[PMID: 35231830]
SW480 IC50
1.1 μM
Compound: 6; AZD-0156
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
[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.

AZD0156 Related Antibodies

Solvant et solubilité
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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
Pureté et documentation
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