Home DNA Damage/DNA Repair ATM/ATR inhibitor - Apoptosis related activator AZD0156 For research use only.

AZD0156

AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities. AZD0156 prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells.

AZD0156 Chemical Structure

AZD0156 Chemical Structure

CAS No. 1821428-35-6

Purity & Quality Control

AZD0156 Related Products

Signaling Pathway

ATM/ATR Signaling Pathways

ATM/ATR Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT29 Function assay 1 hr Inhibition of ATM autophosphorylation at Ser1981 in human HT29 cells preincubated for 1 hr followed by X ray irradiation and measured after 1 hr by Hoechst 33342 dye-based immunofluorescence assay, IC50=0.00057μM 29683659
PC3 Function assay 100 mg/kg 8 hrs Inhibition of Akt phosphorylation at Ser473 in PTEN-deficient human PC3 cells xenograft mouse model at 100 mg/kg, po single dose measured up to 8 hrs 29683659
PC3 Antitumor assay 30 mg/kg Antitumor activity against human PC3 cells xenograft mouse model assessed as inhibition of tumor growth at 30 mg/kg, po bid in presence of 1-aminobenzotriazole 29683659
HT29 Function assay 1 hr Inhibition of ATR in human HT29 cells assessed as decrease in Chk1 phosphorylation at Ser 345 preincubated for 1 hr followed by 4NQO addition and measured after 1 hr by Hoechst 33342 dye-based immunofluorescence assay, IC50=6.2μM 29683659
SW620 Function assay 20 mg/kg Potentiation of tumor regression against human SW620 cells xenografted in immunocompromised mouse at 20 mg/kg, po qd administered on days 2 to 4 of weekly cycle 29683659
HBCx-10 Function assay 5 mg/kg Potentiation of tumor regression against human HBCx-10 cells xenografted in immunocompromised mouse at 5 mg/kg, po qd administered on days 1 to 3 of weekly cycle 29683659
HT29 Function assay Cellular Assay: Assay a) HT29 cells (ECACC #85061109) were seeded into 384 well assay plates (Costar #3712) at a density of 3500 cells/well in 40 μl EMEM medium containing 1% L glutamine and 10% FBS and allowed to adhere overnight. The following morning c, IC50=0.000575μM ChEMBL
MDA-MB-468 Function assay Cellular Assay: Assay d) MDA-MB-468 cells (human breast adenocarcinoma ##ATCC HTB 132) were seeded at 1500 cells/well in 40 μl of DMEM containing 10% FBS and 1% glutamine into Greiner 384 well black flat-bottomed plates, IC50=0.61μM ChEMBL
PC3 Antitumor assay 60 mg/kg Antitumor activity against human PC3 cells xenograft mouse model assessed as inhibition of tumor growth at 60 mg/kg, po bid in presence of 1-aminobenzotriazole ChEMBL
HT29 Function assay Cellular Assay: Assay b) HT29 cells (ECACC #85061109) were seeded into 384 well assay plates (Costar #3712) at a density of 6000 cells/well in 40 μl EMEM medium containing 1% L glutamine and 10% FBS and allowed to adhere overnight, IC50=6.16μM ChEMBL
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Biological Activity

Description AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities. AZD0156 prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells.
Targets
ATM [1]
In vitro
In vitro AZD0156 shows sub-nanomolar potency in cell based assays of ATM inhibition with selectivities of greater than 1000 fold over other members of the PIKK family of enzymes[1].
In Vivo
In vivo AZD0156 is a permeable, highly soluble compound with excellent preclinical pharmacokinetic properties including oral bioavailability. AZD0156 shows robust efficacy in mouse xenograft models after oral administration when combined with DSB inducing agents. AZD0156 is currently undergoing early clinical assessment[1].

Chemical Information & Solubility

Molecular Weight 461.56 Formula

C26H31N5O3
CAS No. 1821428-35-6 SDF Download AZD0156 SDF
Smiles CN1C2=CN=C3C=CC(=CC3=C2N(C1=O)C4CCOCC4)C5=CN=C(C=C5)OCCCN(C)C
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 2 mg/mL

DMSO : 0.3 mg/mL ( (0.64 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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