Home DNA Damage/DNA Repair DNA-PK inhibitor AZD7648 For research use only.

AZD7648

AZD7648 is a potent inhibitor of DNA-PK with an IC50 of 0.6 nM in biochemical assay and more than 100-fold selective against 396 other kinases.

AZD7648 Chemical Structure

AZD7648 Chemical Structure

CAS: 2230820-11-6

Selleck's AZD7648 has been cited by 15 publications

Purity & Quality Control

Batch: Purity: 99.93%
99.93

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Biological Activity

Description AZD7648 is a potent inhibitor of DNA-PK with an IC50 of 0.6 nM in biochemical assay and more than 100-fold selective against 396 other kinases.
Targets
DNA-PK [1]
(Cell-free assay)
0.6 nM
In vitro
In vitro

AZD7648 inhibits IR-induced DNA-PK S2056 auto phosphoryalation with an IC50 = 92 nM in A549 non-small cell lung cancer (NSCLC) cells. In A549 cells, AZD7648 (≥1 µM) in combination with 2Gy IR for 48 hours leads to a significant accumulation of cells arrested in the G2/M of the cell cycle, a 4-fold increase in micronuclei formation, and 3-fold induction of γH2AX, pATM S1981 and 53BP1 foci formation compared with IR alone[2].
Cell Research Cell lines HeLa cells
Concentrations 10 μM
Incubation Time 1 h
Method

Cells were treated with indicated concentration of drug for 1 h.
In Vivo
In vivo

AZD7648 is a potent and highly selective DNA-PK inhibitor, with good crystalline solubility, permeability and metabolic stability, good bioavailability and predictable pharmacokinetics in preclinical species, and potent knockdown of pRPA and regressions in murine xenograft models when combining with olaparib or radiation[1].
Animal Research Animal Models SCID mice
Dosages 4-100 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 380.40 Formula

C18H20N8O2
CAS No. 2230820-11-6 SDF --
Smiles CC1=CC2=NC=NN2C=C1NC3=NC=C4C(=N3)N(C(=O)N4C)C5CCOCC5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 9 mg/mL ( (23.65 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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