product name AZD0156
Description: AZD0156 is an orally bioactive, potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities. AZD0156 inhibits the kinase activity of ATM and ATM-mediated signaling, and prevents DNA damage checkpoint activation, and disrupting DNA damage repair, inducing tumor cell apoptosis, and leading to cell death in ATM-overexpressing tumor cells. AZD0156 was identified as a first in class orally available ATM inhibitor, showing sub-nanomolar potency in cell based assays of ATM inhibition. Moreover, AZD0156 had selectivities of greater than 1000 fold over other members of the PIKK family enzymes.
References: Cancer Res. 2016, 76(14 Suppl):Abstract nr 4859.
461.56
Formula
C26H31N5O3
CAS No.
1821428-35-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: <1 mg/mL
Water: <1 mg/mL
Ethanol: 2 mg/mL (4.3 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: AZD0156 was identified as a first in class orally available ATM inhibitor, showing sub-nanomolar potency in cell based assays of ATM inhibition. Moreover, AZD0156 had selectivities of greater than 1000 fold over other members of the PIKK family enzymes. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In animal study, AZD0156 displayed excellent preclinical PK properties including oral bioavailability. Additionally, in mouse xenograft models, AZD0156 showed robust efficacy after oral administration when combined with double strand breaks (DSB) inducing agents. |
| Animal model | |
| Formulation & Dosage | |
| References | Cancer Res. 2016, 76(14 Suppl):Abstract nr 4859. |
