2. Cell Cycle/DNA Damage PI3K/Akt/mTOR Apoptosis
  3. ATM/ATR Apoptosis
  4. AZD0156

AZD0156 est un inhibiteur puissant, sélectif de ATMet oralement actif avec un IC50 de 0,58 nM. AZD0156 inhibe la signalisation médiée par ATM, empêche l'activation des points de contrôle des dommages à l'ADN, perturbe la réparation des dommages à l'ADN et induit l'apoptosis.

AZD0156 ist ein potenter, selektiver und oral aktiver ATM-Inhibitor mit einem IC50 von 0,58 nM. AZD0156 hemmt den ATM-vermittelten Signalweg, verhindert die Aktivierung von DNA-Schadenskontrollpunkten, unterbricht die Reparatur von DNA-Schäden und induziert die apoptosis. von Tumorzellen.

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.

AZD0156 Chemical Structure

AZD0156 Chemical Structure

CAS No. : 1821428-35-6

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Customer Review

Based on 7 publication(s) in Google Scholar

AZD0156 Related Antibodies

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ATM ATR

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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
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
Clinical Trial
Molecular Weight

461.56

Formula

C26H31N5O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1C2CCOCC2)N(C)C3=C1C4=CC(C5=CC=C(OCCCN(C)C)N=C5)=CC=C4N=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
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)

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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.83%

SDS (393 KB)

COA (248 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References
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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

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.

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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AZD0156 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZD01561821428-35-6AZD 0156AZD-0156ATM/ATRApoptosisAtaxia telangiectasia mutatedATM and RAD3 relatedInhibitorinhibitorinhibit

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