AZ32

SKU: orb1302855

Description

AZ32 is a potent, orally bioavailable, and brain-penetrant small molecule inhibitor of ATM kinase. It demonstrates high enzymatic inhibition (IC50 <6.2 nM) and cellular activity (IC50 = 0.31 µM). This inhibitor is a valuable tool for investigating ATM's role in DNA damage response, cancer research, and in vivo studies of central nervous system malignancies.

Research Area

Molecular Biology, Signal Transduction

Key Properties

• CAS Number: 2288709-96-4
• MW: 328.37
• Purity: 99.94% (May vary between batches)
• Formula: C₂₀H₁₆N₄O
• SMILES: CNC(=O)c1ccc(cc1)-c1cnc2cnc(cn12)-c1ccccc1
• Target: ATM/ATR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.09 mM);DMSO:55 mg/mL (167.49 mM)

Bioactivity

• Target IC50:
  ATM:0.31 μM (in cell)|ATM:6.2 nM
• In Vivo:
  AZ32 exhibits superior blood-brain barrier (BBB) penetration and is more effective as a radiosensitizer in both syngeneic and human orthotopic mouse glioma models compared to AZ31. It acts as a specific inhibitor of the ATM kinase, showcasing commendable BBB penetration in mice. A single oral dose of AZ32 (200 mg/kg) maintains free-brain concentrations above the cellular IC50 for around 22 hours .
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• In Vitro:
  AZ32 is an enhanced blood-brain barrier (BBB)-penetrating ATM inhibitor. AZ32 blocks the DNA damage response and radiosensitized GBM cells in vitro.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, AZ 32, ATR, ATM/ATR, ATM, ATM and RAD3 related, Ataxia telangiectasia mutated, AZ32, AZ-32

Compound Identifiers

PubChem CID

134814488