Identification | Back Directory | [Name]
4-((S)-1-(tetrahydro-2H-pyran-4-yl)ethylamino)-6-(6-(methoxymethyl)pyridin-3-yl)quinoline-3-carboxamide | [CAS]
2088113-98-6 | [Synonyms]
AZ-31 CS-2888 AZ-31;AZ 31 AZ31;AZ-31;AZ 31 4-((S)-1-(tetrahydro-2H-pyran-4-yl)ethylamino)-6-(6-(methoxymethyl)pyridin-3-yl)quinoline-3-carboxamide (S)-6-(6-(methoxymethyl)pyridin-3-yl)-4-((1-(tetrahydro-2H-pyran-4-yl)ethyl)amino)quinoline-3-carboxamide 6-[6-(Methoxymethyl)-3-pyridinyl]-4-[[(1S)-1-(tetrahydro-2H-pyran-4-yl)ethyl]amino]-3-quinolinecarboxamide 3-Quinolinecarboxamide, 6-[6-(methoxymethyl)-3-pyridinyl]-4-[[(1S)-1-(tetrahydro-2H-pyran-4-yl)ethyl]amino]- | [Molecular Formula]
C24H28N4O3 | [MDL Number]
MFCD31922712 | [MOL File]
2088113-98-6.mol | [Molecular Weight]
420.5 |
Chemical Properties | Back Directory | [Boiling point ]
629.8±55.0 °C(Predicted) | [density ]
1.234±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
15.36±0.30(Predicted) | [color ]
Off-white to light yellow |
Hazard Information | Back Directory | [Uses]
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]. | [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. |
| [IC 50]
ATM: 1.2 nM (IC50); ATM: 46 nM (IC50, in cell) | [References]
[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. DOI:10.1158/1535-7163.MCT-17-0975 |
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Company Name: |
BOC Sciences
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Tel: |
1-631-485-4226; 16314854226 |
Website: |
https://www.bocsci.com |
Company Name: |
Twochem Co.Ltd.
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Tel: |
021-58111628 15800915896 |
Website: |
cn.twochem.com |
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