2288709-96-4
AZ32
CAS: 2288709-96-4
Molecular Formula: C20H16N4O
2288709-96-4 - Names and Identifiers
| Name | AZ32 |
| Synonyms | AZ32 N-Methyl-4-(6-phenylimidazo[1,2-a]pyrazin-3-yl)benzamide Benzamide, N-methyl-4-(6-phenylimidazo[1,2-a]pyrazin-3-yl)- |
| CAS | 2288709-96-4 |
2288709-96-4 - Physico-chemical Properties
| Molecular Formula | C20H16N4O |
| Molar Mass | 328.37 |
| Solubility | DMSO : ≥ 150 mg/mL (456.80 mM) |
| Storage Condition | -20℃ |
| Use | AZ32 is an orally available ATM inhibitor that can penetrate the blood-brain barrier with IC50<6.2 nM. ATM is inhibited in cells with IC50 of 0.31 μM. |
| Target | ATM |
| In vitro study | AZ32 is a next-generation blood-brain barrier (BBB)-penetrating ATM inhibitor. AZ32 blocks the DNA damage response and radiosensitized GBM cells in vitro. |
| In vivo study | AZ32, with enhanced BBB penetration, is highly efficient in vivo as radiosensitizer in syngeneic and human, orthotopic mouse glioma model compared with AZ31. AZ32 is a specific inhibitor of the ATM kinase that possesses good BBB penetration in mouse. Following a single oral dose of AZ32 (200 mg/kg) in mice, the free-brain concentrations of AZ32 are in excess of the cellular IC 50 for approximately 22 hours. |
2288709-96-4 - Reference
| Reference Show more | 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. |
2288709-96-4 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.045 ml | 15.227 ml | 30.453 ml |
| 5 mM | 0.609 ml | 3.045 ml | 6.091 ml |
| 10 mM | 0.305 ml | 1.523 ml | 3.045 ml |
| 5 mM | 0.061 ml | 0.305 ml | 0.609 ml |
Last Update：2024-01-02 23:10:35
2288709-96-4 - Reference Information
| biological activity | AZ32 is an orally available ATM inhibitor that penetrates the blood-brain barrier, IC50<6.2 nM. ATM was inhibited in cells with an IC50 of 0.31 μm. |
| Target | ATM 6.2 nM (IC 50 ) ATM 0.31 μm (IC 50 , in cell) |
| in vitro study | AZ32 is a next-generation blood-brain barrier (BBB)-penerating ATM inhibitor. AZ32 blocks the DNA damage response and radiosensitized GBM cells in vitro. |
| in vivo study | AZ32, with enhanced BBB penetration, is highly effective in vivo as radiosentizer in syngenic and human, orthotopic mouse model compared with az31. AZ32 is a specific inhibitor of the ATM kinase that possesses good BBB penetration in mouse. Following a single oral dose of AZ32 (200 mg/kg) in mice, the free-brain concentrations of AZ32 are in excess of the cellular IC 50 for approximately 22 hours. |
Last Update：2024-04-09 21:04:16
