2088113-98-6
2088113-98-6 structure
- Name: AZ31
- Chemical Name: 4-((S)-1-(tetrahydro-2H-pyran-4-yl)ethylamino)-6-(6-(methoxymethyl)pyridin-3-yl)quinoline-3-carboxamide
- CAS Number: 2088113-98-6
- Molecular Formula: C24H28N4O3
- Molecular Weight: 420.50412
- Catalog: Signaling Pathways Cell Cycle/DNA Damage ATM/ATR
- Create Date: 2018-07-08 00:32:47
- Modify Date: 2024-01-10 19:09:02
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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].
| Name | 4-((S)-1-(tetrahydro-2H-pyran-4-yl)ethylamino)-6-(6-(methoxymethyl)pyridin-3-yl)quinoline-3-carboxamide |
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| Synonyms | AZ31 |
| Description | 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]. |
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| Related Catalog | |
| Target |
ATM:1.2 nM (IC50) ATM:46 nM (IC50, in cell) |
| In Vitro | 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]. Western Blot Analysis[1] Cell Line: Human glioma cell line Concentration: 0.3, 1 and 3 μM Incubation Time: 1 hour Result: Blocked phosphorylation of p53-S15, KAP1-S824, and ATM auto-phosphorylation at S1981. Western Blot Analysis[1] Cell Line: H460 and mutant p53 H2228 cell lines Concentration: 10 μM Incubation Time: 1 hour Result: Destabilized p53 of mutant p53 but not wild-type after radiation. |
| In Vivo | AZ31 (50-100 mg/kg; p.o. twice a day) shows low brain coverage[1]. Animal Model: Nude mice[1] Dosage: 50 and 100 mg/kg Administration: Oral gavage; 50 and 100 mg/kg twice a day Result: Exhibited exposure over IC50 at 0.046 μM in brain only for 2-3 hours. |
| References |
| Molecular Formula | C24H28N4O3 |
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| Molecular Weight | 420.50412 |
| Storage condition | -20℃ |
| Hazard Codes | N |
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