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

Batch: S855601 Purity: 98.63%
98.63

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 add μL Corn oil, mix and clarify.

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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

Mechanism of Action

Targets/IC50/Ki
ATM
In vitro

Antitumor effects of AZ31 + SN38 are cytostatic rather than cytotoxic.
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.
References

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