Home DNA Damage/DNA Repair DNA-PK inhibitor AZD7648

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AZD7648 DNA-PK inhibitor

Cat.No.S8843

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 DNA-PK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 380.40

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Quality Control

Batch: Purity: 99.93%
99.93

Solubility

In vitro
Batch:

DMSO : 9 mg/mL (23.65 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous 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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 380.40 Formula

C18H20N8O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2230820-11-6 -- Storage of Stock Solutions

Synonyms N/A Smiles CC1=CC2=NC=NN2C=C1NC3=NC=C4C(=N3)N(C(=O)N4C)C5CCOCC5

Mechanism of Action

Targets/IC50/Ki
DNA-PK
(Cell-free assay)
0.6 nM
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, this compound (≥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.
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 AZD2281 or radiation.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/31699977/

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