AZD7648

Catalog No.S8843 Batch:S884303

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Technical Data

Formula

C18H20N8O2
Molecular Weight 380.40 CAS No. 2230820-11-6
Solubility (25°C)* In vitro DMSO 9 mg/mL (23.65 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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].
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[1].

Protocol (from reference)

Cell Assay:

[3]
  • Cell lines

    HeLa cells

  • Concentrations

    10 μM

  • Incubation Time

    1 h

  • Method

    Cells were treated with indicated concentration of drug for 1 h.
Animal Study:

[4]
  • Animal Models

    SCID mice

  • Dosages

    4-100 mg/kg

  • Administration

    p.o.

Selleck's AZD7648 has been cited by 16 publications

Different Impacts of DNA-PK and mTOR Kinase Inhibitors in Combination with Ionizing Radiation on HNSCC and Normal Tissue Cells [ Cells, 2024, 13(4)304] PubMed: 38391917
Negative feedback regulation of MAPK signaling is an important driver of chronic lymphocytic leukemia progression [ Cell Rep, 2023, 42(10):113017] PubMed: 37792532
Phosphatases maintain low catalytic activity of SGK1: DNA damage resets the balance in favor of phosphorylation [ J Biol Chem, 2023, S0021-9258(23)01969-5] PubMed: 37343701
Synergistic cytotoxicity of fludarabine, clofarabine, busulfan, vorinostat and olaparib in AML cells [ Front Oncol, 2023, 13:1287444] PubMed: 38074694
Inhibition of DNA-dependent protein kinase catalytic subunit boosts rAAV transduction of polarized human airway epithelium [ Mol Ther Methods Clin Dev, 2023, 31:101115] PubMed: 37841417
Disparate pathways for extrachromosomal DNA biogenesis and genomic DNA repair [ bioRxiv, 2023, 2023.10.22.563489] PubMed: 37961138
MEK inhibition overcomes chemoimmunotherapy resistance by inducing CXCL10 in cancer cells [ Cancer Cell, 2022, S1535-6108(21)00662-0] PubMed: 35051357
TDP1-independent pathways in the process and repair of TOP1-induced DNA damage [ Nat Commun, 2022, 13(1):4240] PubMed: 35869071
DNA-PKcs promotes fork reversal and chemoresistance [ Mol Cell, 2022, 82-20:3932-3942.e6] PubMed: 36130596
Effective Radiosensitization of Bladder Cancer Cells by Pharmacological Inhibition of DNA-PK and ATR [ Biomedicines, 2022, 10(6)1277] PubMed: 35740300

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.