1. Cell Cycle/DNA Damage PI3K/Akt/mTOR Apoptosis
  2. DNA-PK ATM/ATR PI3K Apoptosis
  3. AZD-7648

AZD-7648 is a potent, orally active, selective DNA-PK inhibitor with an IC50 of 0.6 nM. AZD-7648 induces apoptosis and shows antitumor activity.

For research use only. We do not sell to patients.

CAS No. : 2230820-11-6

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Customer Review

Based on 48 publication(s) in Google Scholar

Other Forms of AZD-7648:

Top Publications Citing Use of Products

48 Publications Citing Use of MCE AZD-7648

Flow Cytometry
Cell Proliferation/Viability Assay
Apoptosis Analysis
Cell Imaging/Staining

    AZD-7648 purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2025 Aug 11;53(15):gkaf767.  [Abstract]

    AZD7648 (1 µM; 48 h) showed less cytotoxicity in HSPCs relative to M3814 (2 µM; 48 h).

    AZD-7648 purchased from MedChemExpress. Usage Cited in: Theranostics. 2023 Aug 28;13(14):4745-4761.  [Abstract]

    Cell growth response at Day 14, shown as % relative growth as compared to control of H1299-7 cells treated with 0, 5 or 10 MBq/mL LuTate alone, or in combination with 0.5 μM or 1 μM of AZD-7648.

    AZD-7648 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2023 Oct 18;24(20):15331.

    Log dose–response viability curve of AZD-7648 after 24 or 48 (KG-1*) hours of treatment.

    AZD-7648 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2023 Oct 18;24(20):15331.

    Analysis of cell death induced by AZD-7648 (AZD,50-200 μM) in CML and AML cell lines after 24 or 48 (KG-1) hours of treatment.The type of cell death was identified using annexin V/propidium iodide staining and analyzed using flow cytometry. Data are expressed as a percentage (%) of viable, early apoptosis, late apoptosis/necrotic, and necrotic cells and represent mean ± SEM of 5 independent experiments. Statistical analyses were performed by comparison with control, using one-way ANOVA and Dunnett’s multiple comparisons test, Kruskal–Wallis and Dunn’s multiple comparisons test, unpaired t-test, or Mann–Whitney test.

    AZD-7648 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2023 Oct 18;24(20):15331.

    Analysis of cell death induced by AZD-7648 (AZD, 50-200 μM) in CML and AML cell lines after 24 or 48 (KG-1) hours of treatment. Cell morphology was observed by light microscopy (amplification: 1000×), and the most representative image was selected.

    AZD-7648 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Sep 8;13(1):5295.  [Abstract]

    HEK 293T DSB-Spectrum_V3 cells were transfected with Cas9 and an sgRNA targeting either AAVS1 or BFP, followed by treatment with the DNA-PKcs inhibitors M3841 (2 µM) or AZD7648 (2 µM). At 72h after Cas9 transfection cells were analyzed by flow cytometry (n=4; mean ± SEM; One-way ANOVA, post-hoc Dunnett's).

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    AZD-7648 is a potent, orally active, selective DNA-PK inhibitor with an IC50 of 0.6 nM. AZD-7648 induces apoptosis and shows antitumor activity[1].

    IC50 & Target[1]

    PI3Kγ

    1.37 μM (IC50)

    ATM

    17.93 μM (IC50)

    DNA-PKcs

    91.3 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    0.091 μM
    Compound: Example 16; AZD7648
    Inhibition of DNA-PK in human A549 cells assessed as reduction in irradiation-induced autophosphorylation at S2056 residue preincubated for 1 hr followed by 8 Gy irradiation and measured after 1 hr by ELISA
    Inhibition of DNA-PK in human A549 cells assessed as reduction in irradiation-induced autophosphorylation at S2056 residue preincubated for 1 hr followed by 8 Gy irradiation and measured after 1 hr by ELISA
    [PMID: 31851518]
    B16-F10 IC50
    11.4 μM
    Compound: AZD-7648
    Synergistic antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs in presence of doxorubicin by CCK-8 assay
    Synergistic antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs in presence of doxorubicin by CCK-8 assay
    [PMID: 38587857]
    B16-F10 IC50
    33.6 μM
    Compound: AZD-7648
    Antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
    Antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
    [PMID: 38587857]
    CHO IC50
    > 198 μM
    Compound: Example 16; AZD7648
    Inhibition of human ERG stably expressed in CHO cells at -90 mV holding potential by electrophysiological assay
    Inhibition of human ERG stably expressed in CHO cells at -90 mV holding potential by electrophysiological assay
    [PMID: 31851518]
    CT26 IC50
    18.8 μM
    Compound: AZD-7648
    Antiproliferative activity against mouse CT26 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
    Antiproliferative activity against mouse CT26 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
    [PMID: 38587857]
    CT26 IC50
    6.74 μM
    Compound: AZD-7648
    Synergistic antiproliferative activity against mouse CT26 cells assessed as reduction in cell viability incubated for 48 hrs in presence of doxorubicin by CCK-8 assay
    Synergistic antiproliferative activity against mouse CT26 cells assessed as reduction in cell viability incubated for 48 hrs in presence of doxorubicin by CCK-8 assay
    [PMID: 38587857]
    HCT-116 IC50
    19.5 μM
    Compound: AZD-7648
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of 100 nM doxorubicin by MTT assay
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of 100 nM doxorubicin by MTT assay
    [PMID: 35468512]
    HCT-116 IC50
    35.3 μM
    Compound: AZD-7648
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    [PMID: 35468512]
    HCT-116 IC50
    38.08 nM
    Compound: 4; AZD7648
    Inhibition of colony formation in human HCT-116 cells preincubated with compound for 1 hr followed by exposure to 2 Gy gamma irradiation and measured after 7 days by crystal violet staining based chemiluminescence assay
    Inhibition of colony formation in human HCT-116 cells preincubated with compound for 1 hr followed by exposure to 2 Gy gamma irradiation and measured after 7 days by crystal violet staining based chemiluminescence assay
    [PMID: 38117951]
    HT-29 IC50
    17.9 μM
    Compound: Example 16; AZD7648
    Inhibition of ATM in human HT-29 cells assessed as reduction in irradiation-induced autophosphorylation at Ser1981 residue preincubated for 1 hr followed by 6 Gy irradiation and measured after 1 hr by Hoechst staining-based imaging analysis
    Inhibition of ATM in human HT-29 cells assessed as reduction in irradiation-induced autophosphorylation at Ser1981 residue preincubated for 1 hr followed by 6 Gy irradiation and measured after 1 hr by Hoechst staining-based imaging analysis
    [PMID: 31851518]
    HT-29 IC50
    > 29 μM
    Compound: Example 16; AZD7648
    Inhibition of ATR in human HT-29 cells assessed as reduction in 4NQO-induced CHK1 phosphorylation at S345 residue preincubated for 1 hr followed by 4NQO addition and measured after 1 hr by Hoechst staining-based imaging analysis
    Inhibition of ATR in human HT-29 cells assessed as reduction in 4NQO-induced CHK1 phosphorylation at S345 residue preincubated for 1 hr followed by 4NQO addition and measured after 1 hr by Hoechst staining-based imaging analysis
    [PMID: 31851518]
    HeLa IC50
    0.6 nM
    Compound: Example 16; AZD7648
    Inhibition of human HeLa cell-derived full length DNA-PK catalytic subunit using fluorescein-EPPLSQEAFADLWKK as substrate preincubated for 30 mins followed by substrate addition and measured after 40 mins TR-FRET assay
    Inhibition of human HeLa cell-derived full length DNA-PK catalytic subunit using fluorescein-EPPLSQEAFADLWKK as substrate preincubated for 30 mins followed by substrate addition and measured after 40 mins TR-FRET assay
    [PMID: 31851518]
    Jurkat IC50
    0.09 μM
    Compound: AZD-7648
    Synergistic antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 48 hrs in presence of doxorubicin by CCK-8 assay
    Synergistic antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 48 hrs in presence of doxorubicin by CCK-8 assay
    [PMID: 38587857]
    Jurkat IC50
    12.3 μM
    Compound: AZD-7648
    Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
    Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
    [PMID: 38587857]
    MDA-MB-231 IC50
    > 30 μM
    Compound: Example 16; AZD7648
    Inhibition of mTOR/PI3Kalpha in human MDA-MB-231 cells assessed as reduction in AKT phosphorylation at S473 residue measured after 2 hrs by Hoechst staining-based imaging analysis
    Inhibition of mTOR/PI3Kalpha in human MDA-MB-231 cells assessed as reduction in AKT phosphorylation at S473 residue measured after 2 hrs by Hoechst staining-based imaging analysis
    [PMID: 31851518]
    MDA-MB-468 IC50
    > 30 μM
    Compound: Example 16; AZD7648
    Inhibition of PI3Kbeta in human MDA-MB-468 cells assessed as reduction in AKT phosphorylation at T208 residue measured after 2 hrs by QuantaBlu substrate based fluorescence assay
    Inhibition of PI3Kbeta in human MDA-MB-468 cells assessed as reduction in AKT phosphorylation at T208 residue measured after 2 hrs by QuantaBlu substrate based fluorescence assay
    [PMID: 31851518]
    In Vitro

    AZD7648 (0-30 μM) is a potent radiosensitizer[1].
    AZD7648 (3 μM) increases sensitivity to Doxorubicin (HY-15142A)[1].
    AZD7648 (0.6 μM) enhances the activity of PARP inhibitor Olaparib (HY-10162)[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Cycle Analysis[1]

    Cell Line: IR (ionizing radiation)-treated A549 cells or A549 cells
    Concentration: 0-30 μM
    Incubation Time: 48 h
    Result: Arrested cell cycle at G2/M phase.

    Western Blot Analysis[1]

    Cell Line: IR (ionizing radiation)-treated A549 cells or OAW42 cells treated with Doxorubicin
    Concentration: 0.03, 0.1, 0.3, 1, 3, 10 and 30 μM for A549; 3 μM for OAW42
    Incubation Time: 1 h for A549; 0.5, 2, 4, 8 and 16 h for OAW42
    Result: Potently inhibited DNA-PKcs autophosphorylation at Ser2056. Downregulated pDNA-PKcs Ser2056, γH2AX Ser139 and pRPA32 Ser4/Ser8 phosphorylation at early time points (at 30 min, 2 h and 4 h).
    Resulted in increased levels of γH2AX and the apoptosis marker cleaved PARP1 compared with doxorubicin treatment alone at later time points (8 and 16 h).
    In Vivo

    AZD-7648 (100 mg/kg; p.o.; once daily for 5 days) induces tumour growth inhibition and tumour regression[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Nude mice, A549 xenografts and NCI-H1299 xenografts[1]
    Dosage: 100 mg/kg
    Administration: Oral administration, once daily for 5 days
    Result: Induced tumour growth inhibition in combination with IR in A549 xenografts and induced tumour regression in combination with IR in NCI-H1299 xenografts.
    Molecular Weight

    380.40

    Formula

    C18H20N8O2

    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    CC1=CC2=NC=NN2C=C1NC3=NC=C(N(C)C(N4C5CCOCC5)=O)C4=N3

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 5.83 mg/mL (15.33 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6288 mL 13.1441 mL 26.2881 mL
    5 mM 0.5258 mL 2.6288 mL 5.2576 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    In Vivo:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  0.5% HPMC/0.1% Tween-80 in Saline water

      Solubility: 10 mg/mL (26.29 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
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    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.86%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.6288 mL 13.1441 mL 26.2881 mL 65.7203 mL
    5 mM 0.5258 mL 2.6288 mL 5.2576 mL 13.1441 mL
    10 mM 0.2629 mL 1.3144 mL 2.6288 mL 6.5720 mL
    15 mM 0.1753 mL 0.8763 mL 1.7525 mL 4.3814 mL
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    Product Name:
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