4-((S)-1-(tetrahydro-2H-pyran-4-yl)ethylamino)-6-(6-(methoxymethyl)pyridin-3-yl)quinoline-3-carboxamide
4-((S)-1-(tetrahydro-2H-pyran-4-yl)ethylamino)-6-(6-(methoxymethyl)pyridin-3-yl)quinoline-3-carboxamide Basic information
- Product Name:
- 4-((S)-1-(tetrahydro-2H-pyran-4-yl)ethylamino)-6-(6-(methoxymethyl)pyridin-3-yl)quinoline-3-carboxamide
- Synonyms:
-
- 4-((S)-1-(tetrahydro-2H-pyran-4-yl)ethylamino)-6-(6-(methoxymethyl)pyridin-3-yl)quinoline-3-carboxamide
- AZ-31
- AZ-31;AZ 31
- (S)-6-(6-(methoxymethyl)pyridin-3-yl)-4-((1-(tetrahydro-2H-pyran-4-yl)ethyl)amino)quinoline-3-carboxamide
- AZ31;AZ-31;AZ 31
- CS-2888
- 3-Quinolinecarboxamide, 6-[6-(methoxymethyl)-3-pyridinyl]-4-[[(1S)-1-(tetrahydro-2H-pyran-4-yl)ethyl]amino]-
- 6-[6-(Methoxymethyl)-3-pyridinyl]-4-[[(1S)-1-(tetrahydro-2H-pyran-4-yl)ethyl]amino]-3-quinolinecarboxamide
- CAS:
- 2088113-98-6
- MF:
- C24H28N4O3
- MW:
- 420.5
- Mol File:
- 2088113-98-6.mol
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4-((S)-1-(tetrahydro-2H-pyran-4-yl)ethylamino)-6-(6-(methoxymethyl)pyridin-3-yl)quinoline-3-carboxamide Chemical Properties
- Boiling point:
- 629.8±55.0 °C(Predicted)
- Density
- 1.234±0.06 g/cm3(Predicted)
- pka
- 15.36±0.30(Predicted)
- form
- Solid
- color
- Off-white to light yellow
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4-((S)-1-(tetrahydro-2H-pyran-4-yl)ethylamino)-6-(6-(methoxymethyl)pyridin-3-yl)quinoline-3-carboxamide Usage And Synthesis
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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