Biochem/physiol Actions
AZ32 is an orally active, potent and selective ataxia telangiectasia mutated (ATM) kinase inhibitor (IC50 ﹤6.2 nM; DNA-PK & PI3Ka IC50 =4.6 µM, hERG IC50 = 17.6 µM) with good aqueous solubility (24 µM) and blood-brain barrier (BBB) permeability in mice (free brain/plasma ratio = 0.26; 200 mg/kg p.o.). AZ32 exhibits radiosensitizing efficacy in human & murine glioma cultures by blocking radiation-induced DNA damage response (ATM pS1981 IC50 = 310 nM; 100% blockage of KAP1 pS824 & p53 pS15 at 300 nM; T98G cells). AZ32 (200 mg/kg/day p.o.) improves whole-head irradiation treatment survival rate among mice with brain GL261 tumors or NCI-H2228 NSCLC metastases in vivo.
| Colour | white to beige |
|---|---|
| Manufacturer | SIGMA-ALDRICH |
| Storage Temp. | 2-8°C |
| Solubility | DMSO: 2 mg/mL, clear |
| Form | powder |
| Assay | ≥98% (HPLC) |
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