Home DNA Damage/DNA Repair ATM/ATR inhibitor AZ31

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AZ31 ATM/ATR inhibitor

Cat.No.S8556

AZ31 is a selective and novel ATM inhibitor with an IC50 of <0.0012 μM. It shows excellent selectivity over closely related enzymes (>500 fold selective over DNA-PK and PI3Kα and >1000 fold selective over mTOR, PI3Kβ and PI3Kγ).
AZ31 ATM/ATR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 420.50

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Quality Control

Chemical Information, Storage & Stability

Molecular Weight 420.50 Formula

C24H28N4O3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2088113-98-6 -- Storage of Stock Solutions

Synonyms N/A Smiles CC(C1CCOCC1)NC2=C3C=C(C=CC3=NC=C2C(=O)N)C4=CN=C(C=C4)COC

Solubility

In vitro
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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Mechanism of Action

Targets/IC50/Ki
ATM [2]
In vitro

Antitumor effects of AZ31 + SN38 are cytostatic rather than cytotoxic[1].
Kinase Assay
ATM enzyme assay
Compounds in 100% DMSO were added to assay plates by acoustic dispensing. ATM enzyme was added in a Hepes buffer (50 mM HEPES pH 7.4, 150 mM NaCl, 10 mM, MnCl2 1 mM, DTT, 5% v/v Glycerol, 0.05% v/v Tween 20) and allowed to preincubate with compound for 30 minutes prior to addition of substrate solution containing p53 and ATP. The enzyme reaction was stopped after 2 hours by the addition of detection reagent (33 mM HEPES pH 7.4, 20 mM EDTA, 0.1 M KF, 0.1 mg/mL BSA, 13 nM D2 Anti-GST antibody (Cisbio) and 0.5 nM Eu3+ Anti-p53phosphoS15 antibody) and incubated overnight before reading on a Pherastar Instrument with a standard HTRF filter block method. The final concentrations of DMSO, ATP and p53 in the assay were 1%, 5 µM, and 50 nM respectively. IC50 values (concentrations of test compound that inhibited 50% of enzyme activity) were determined using a four parameter fit method (smart fitting model) in the data analysis software.
In vivo

Pharmacokinetic investigation of AZ31 as a single agent and in combination with irinotecan revealed that plasma concentrations of this compound were highest 1-hour after administration followed by a stepwise decrease at 3, 6 and 16 hour in the combination sensitive CRC098[1].
References

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