2. Cell Cycle/DNA Damage PI3K/Akt/mTOR
  3. ATM/ATR
  4. AZ31

AZ31 is a a potent, highly selective, and orally active ATM inhibitor with an IC50 of <1.2 nM for ATM enzyme, and an IC50 of 46 nM for ATM in cell. AZ31 shows excellent selectivity over ATR (>500-fold) and excellent PIKK-family selectivity and pan-kinase selectivity. AZ31 is a potent radiosensitizer in vitro, it can be used for the research of cancer.

For research use only. We do not sell to patients.

AZ31 Chemical Structure

AZ31 Chemical Structure

CAS No. : 2088113-98-6

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5 mg USD 130 In-stock
10 mg USD 210 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

AZ31 is a a potent, highly selective, and orally active ATM inhibitor with an IC50 of <1.2 nM for ATM enzyme, and an IC50 of 46 nM for ATM in cell. AZ31 shows excellent selectivity over ATR (>500-fold) and excellent PIKK-family selectivity and pan-kinase selectivity. AZ31 is a potent radiosensitizer in vitro, it can be used for the research of cancer[1].

IC50 & Target[1]

ATM

1.2 nM (IC50)

ATM

46 nM (IC50, in cell)

In Vitro

AZ31 (0.3-3 μM; 1 h) affects phosphorylation of a panel of ATM targets[1].
AZ31 (10 μM; 1 h) affects stabilization of p53 in H2228 lung cancer cells after radiation[1].

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

AZ31 Related Antibodies

Western Blot Analysis[1]

Cell Line: Human glioma cell line
Concentration: 0.3, 1 and 3 μM
Incubation Time: 1 hour
Result: Blocked phosphorylation of p53-S15, KAP1-S824, and ATM auto-phosphorylation at S1981.

Western Blot Analysis[1]

Cell Line: H460 and mutant p53 H2228 cell lines
Concentration: 10 μM
Incubation Time: 1 hour
Result: Destabilized p53 of mutant p53 but not wild-type after radiation.
In Vivo

AZ31 (50-100 mg/kg; p.o. twice a day) shows low brain coverage[1].

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

Animal Model: Nude mice[1]
Dosage: 50 and 100 mg/kg
Administration: Oral gavage; 50 and 100 mg/kg twice a day
Result: Exhibited exposure over IC50 at 0.046 μM in brain only for 2-3 hours.
Molecular Weight

420.50

Formula

C24H28N4O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=C(N[C@@H](C)C2CCOCC2)C3=CC(C4=CC=C(COC)N=C4)=CC=C3N=C1)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (237.81 mM; Need ultrasonic; 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 2.3781 mL 11.8906 mL 23.7812 mL
5 mM 0.4756 mL 2.3781 mL 4.7562 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3781 mL 11.8906 mL 23.7812 mL 59.4530 mL
5 mM 0.4756 mL 2.3781 mL 4.7562 mL 11.8906 mL
10 mM 0.2378 mL 1.1891 mL 2.3781 mL 5.9453 mL
15 mM 0.1585 mL 0.7927 mL 1.5854 mL 3.9635 mL
20 mM 0.1189 mL 0.5945 mL 1.1891 mL 2.9727 mL
25 mM 0.0951 mL 0.4756 mL 0.9512 mL 2.3781 mL
30 mM 0.0793 mL 0.3964 mL 0.7927 mL 1.9818 mL
40 mM 0.0595 mL 0.2973 mL 0.5945 mL 1.4863 mL
50 mM 0.0476 mL 0.2378 mL 0.4756 mL 1.1891 mL
60 mM 0.0396 mL 0.1982 mL 0.3964 mL 0.9909 mL
80 mM 0.0297 mL 0.1486 mL 0.2973 mL 0.7432 mL
100 mM 0.0238 mL 0.1189 mL 0.2378 mL 0.5945 mL
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AZ31 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:

AZ312088113-98-6AZ 31AZ-31ATM/ATRAtaxia telangiectasia mutatedATM and RAD3 relatedradiosensitizerhuman gliomap53auto-phosphorylationKAP1-S824brain coveragemiceInhibitorinhibitorinhibit

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