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AZD-0156

Names

[ CAS No. ]:
1821428-35-6

[ Name ]:
AZD-0156

[Synonym ]:
8-{6-[3-(Dimethylamino)propoxy]-3-pyridinyl}-3-methyl-1-(tetrahydro-2H-pyran-4-yl)-1,3-dihydro-2H-imidazo[4,5-c]chinolin-2-on
2H-Imidazo[4,5-c]quinolin-2-one, 8-[6-[3-(dimethylamino)propoxy]-3-pyridinyl]-1,3-dihydro-3-methyl-1-(tetrahydro-2H-pyran-4-yl)-
8-{6-[3-(Dimethylamino)propoxy]-3-pyridinyl}-3-methyl-1-(tetrahydro-2H-pyran-4-yl)-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one
8-{6-[3-(Diméthylamino)propoxy]-3-pyridinyl}-3-méthyl-1-(tétrahydro-2H-pyran-4-yl)-1,3-dihydro-2H-imidazo[4,5-c]quinoléin-2-one
AZD-0156
AZD0156

Biological Activity

[Description]:

AZD0156 is an oral, potent and selective ATM inhibitor with an IC50 of 0.58 nM.

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> ATM/ATR
Signaling Pathways >> PI3K/Akt/mTOR >> ATM/ATR
Research Areas >> Cancer

[Target]

ATM


[In Vitro]

AZD0156 inhibits the kinase activity of ATM and ATM-mediated signaling, prevents DNA damage checkpoint activation, and disrupts DNA damage repair, inducs tumor cell apoptosis, and leads to cell death in ATM-overexpressing tumor cells[1].

[Cell Assay]

HT29 cells are seeded into 384 well assay plates at a density of 6000 cells/well in 40 μL EMEM medium containing 1% L glutamine and 10% FBS and allowed to adhere overnight. The following morning compound of Formula (I) in 100% DMSO is added to assay plates by acoustic dispensing. After lh incubation at 37°C and 5% C02, 40 nL of 3 mM 4NQO in 100% DMSO is added to all wells by acoustic dispensing, except minimum control wells which are left untreated with 4NQO to generate a null response control. Plates are returned to the incubator for a further lh. Then cells are fixed by adding 20 μL of 3.7% formaldehyde in PBS solution and incubating for 20 mins at r.t.. Then 20 μL of 0.1% Triton XI 00 in PBS is added and incubated for 10 minutes at r.t., to permeabalise cells. Then the plates are washed once with 50 μL/well PBS, using a Biotek EL405 plate washer.

[References]

[1]. Imidazo[4,5-c]quinolin-2-one compounds and their use in treating cancer.?


[Related Small Molecules]

Wortmannin | Ceralasertib(AZD6738) | Berzosertib (VE-822) | KU55933 (ATM Kinase Inhibitor) | VE-821 | KU 60019 | AZ20 | AZD1390 | CP-466722 | CGK 733 | ETP-46464 | KU 59403

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
628.3±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C26H31N5O3

[ Molecular Weight ]:
461.556

[ Flash Point ]:
333.8±31.5 °C

[ Exact Mass ]:
461.242676

[ LogP ]:
2.40

[ Appearance of Characters ]:
white solid

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.626

[ Storage condition ]:
-20℃

Related Compounds