For research use only. Not for therapeutic Use.
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].
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].
AZ31 (50-100 mg/kg; p.o. twice a day) shows low brain coverage[1].
| Catalog Number | I022801 |
| CAS Number | 2088113-98-6 |
| Synonyms | 6-[6-(methoxymethyl)pyridin-3-yl]-4-[[(1S)-1-(oxan-4-yl)ethyl]amino]quinoline-3-carboxamide |
| Molecular Formula | C24H28N4O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H28N4O3/c1-15(16-7-9-31-10-8-16)28-23-20-11-17(18-3-5-19(14-30-2)26-12-18)4-6-22(20)27-13-21(23)24(25)29/h3-6,11-13,15-16H,7-10,14H2,1-2H3,(H2,25,29)(H,27,28)/t15-/m0/s1 |
| InChIKey | DISRGUXSEDBDDN-HNNXBMFYSA-N |
| SMILES | CC(C1CCOCC1)NC2=C3C=C(C=CC3=NC=C2C(=O)N)C4=CN=C(C=C4)COC |
| Reference | [1]. Karlin J, et al. Orally Bioavailable and Blood-Brain Barrier-Penetrating ATM Inhibitor (AZ32) Radiosensitizes Intracranial Gliomas in Mice. Mol Cancer Ther. 2018 Aug;17(8):1637-1647. |
