My cart
In the shopping cart is not goods, to choose and buy!
  • Product Name
  • Size
  • Quantity
  • Amount
    Selected items : 0 pieces Total : CHECK OUT()
    NU7441 (KU57788)
    NU7441 (KU57788)

    Price:
    Market Price:

    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V0108
    CAS #: 503468-95-9Purity ≥98%

    Description: NU7441 (also called KU-57788) is a highly potent, selective and ATP-competitive inhibitor of DNA-PK (DNA-dependent protein kinase) with IC50 of 14 nM, has anticancer activity. It also inhibits PI3K with IC50 value of 5 μM in cell-free assays. NU7441 showed no inhibition effect on the DNA-PK-related enzymes ATM and ATR at concentration of 100 μM. For mTOR and PI3K, NU7441 exhibited inhibition activities with IC50 values of 1.7 and 5 μM, respectively, which were about 100-fold higher than the IC50 value of DNA-PK. NU7441 sensitized HeLa cells to ionizing radiation in vitro, with dose modification factors of 2.5 at 10% survival being observed at 0.5 microM. 

    References: J Med Chem. 2005 Dec 1;48(24):7829-46; Cancer Res. 2006 May 15;66(10):5354-62.

    Customer Validation
    Official Supplier of
    • VE
    • OF
    • YALE
    • hhmi
    • 香港大学
    Related Products
    Publications Citing InvivoChem Products
    • Physicochemical and Storage Information
    • Protocol
    • Quality Control Documentation
    • Related Biological Data
    • Customer Review

    Molecular Weight (MW)

    413.49

    Formula

    C25H19NO3S

    CAS No.

    503468-95-9

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 4 mg/mL warming (9.7 mM)

    Water:<1 mg/mL (slightly soluble or insoluble)

    Ethanol: <1 mg/mL (slightly soluble or insoluble)

    Solubility (In vivo)

    4% DMSO+30% PEG 300+5% Tween 80+ddH2O: 1.0 mg/mL

    Synonym

    KU-57788; KU 57788; KU57788; NU7441; NU-7441; NU 7441

    SMILES Code

    O=C1C=C(N2CCOCC2)OC3=C(C4=C5C(C6=CC=CC=C6S5)=CC=C4)C=CC=C13

    Chemical Name

    8-dibenzothiophen-4-yl-2-morpholin-4-ylchromen-4-one


    • Molarity Calculator
    • Dilution Calculator
    • The molarity calculator equation

      Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

      • Mass
      • Concentration
      • Volume
      • Molecular Weight *
      • =
      • ×
      • ×
    • The dilution calculator equation

      Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

      This equation is commonly abbreviated as: C1V1 = C2V2

      • Concentration (start)
      • ×
      • Volume (start)
      • =
      • Concentration (final)
      • ×
      • Volume (final)
      • ×
      • =
      • ×
      • C1
      •  
      • V1
      •  
      • C2
      •  
      • V2

    In Vitro

    In Vitro Activity: NU7441 (also called KU-57788) is a highly potent, selective and ATP-competitive DNA-PK inhibitor with IC50 of 14 nM. It also inhibits PI3K with IC50 value of 5 μM in cell-free assays. NU7441 showed no inhibition effect on the DNA-PK-related enzymes ATM and ATR at concentration of 100 μM. For mTOR and PI3K, NU7441 exhibited inhibition activities with IC50 values of 1.7 and 5 μM, respectively, which were about 100-fold higher than the IC50 value of DNA-PK. NU7441 sensitized HeLa cells to ionizing radiation in vitro, with dose modification factors of 2.5 at 10% survival being observed at 0.5 microM. 

     

    Kinase Assay:NU7441 (also called KU-57788) is a highly potent, selective and ATP-competitive DNA-PK inhibitor with IC50 of 14 nM. It also inhibits PI3K with IC50 value of 5 μM in cell-free assays.  

     

    Cell Assay: SW620, LoVo, V3-YAC and V3 cells; The effect of NU7441 on cellular survival following exposure to etoposide, doxorubicin, and ionizing radiation is measured in SW620, LoVo, V3, and V3-YAC cells by clonogenic assays. Briefly, growing cells in six-well plates or 6-cm dishes are exposed to etoposide or doxorubicin with or without NU7441 (0.5 or 1.0 μM) for 16 hours. For radiosensitization studies, NU7441 is added to the cells 1 hour before irradiation. V3 and V3-YAC cells are exposed to γ-irradiation (3.1 Gy/min 137Cesium). SW620 and LoVo are exposed to X-irradiation (2.9 Gy/min at 230 kV, 10 mA) due to the equipment available. After irradiation, the cells are incubated with or without NU7441 for a further 16 hours. Cells are then harvested by trypsinization, counted, and seeded into 10-cm diameter Petri dishes at densities varying from 100 to 105 per dish in drug-free medium for colony formation. Colonies are stained with crystal violet after 10 to 14 days and counted with an automated colony counter. The survival reduction factor (SRF) is calculated as the surviving fraction of cells in the absence of NU7441 divided by the surviving fraction of cells in the presence of NU7441 for any given dose or concentration of cytotoxic agent. The dose modification ratio (DMR90) is calculated as the concentration/dose of cytotoxic agent required to kill 90% of the cells in the absence of NU7441 divided by the concentration/dose of cytotoxic agent required to kill 90% of the cells in the presence of NU7441.

    NU7441 increases the persistence of γH2AX foci after ionizing radiation–induced or etoposide-induced DNA damage. NU7441 (0.5 μM or 1 μM) appreciably increases G2-M accumulation induced by ionizing radiation, etoposide, and doxorubicin in both SW620 and LoVo cells. NU7441 causes persistence of doxorubicin- and ionising radiation-induced DNA double-strand break and also slightly decreases homologous recombination activity DNA-PK-proficient M059-Fus-1 and DNA-PK-deficient M059 J human tumour cells. NU7441 inhibits UV-induced RPA p34 hyperphosphorylation in a dose-dependent manner both in cells lacking and cells expressing polymerase η. NU7441 increases levels of fludarabine-induced γH2AX foci and correspondingly decreased fludarabine-induced cell death in chronic lymphocytic leukemia cells. NU7441 also inhibits mitoxantrone-induced DNA-PKcs autophosphorylation and repair in chronic lymphocytic leukemia cells.

    In Vivo

    NU7441 intraperitoneally administrated at dose of 10 mg/kg maintains for at least 4 hours shows nontoxic and increases etoposide-induced tumor growth delay 2-fold in mice bearing SW620 xenografts.

    Animal model

    Female rude mice bearing SW620 xenografts

    Formulation & Dosage

    Solubilized in 0.9% sodium chloride solution; 10 mg/kg; i.p.

    References

    [1] Leahy JJ, et al. Bioorg Med Chem Lett, 2004, 14(24), 6083-6087. ;[2] Zhao Y, et al. Cancer Res, 2006 , 66(10), 5354-5362.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    NU7441 (KU-57788)

    NU7441 (0.3 μM) enhances cellular senescence in irradiated H1299 cells.  2016 Sep;107(9):1250-5.

    NU7441 (KU-57788)

    Both X‐rays and carbon ions induce radio‐sensitization in non‐small cell lung cancer (NSCLC) cells with nontoxic conce ntrations of NU7441 treatment.   2016 Sep;107(9):1250-5.

    NU7441 (KU-57788)

    Non‐small cell lung cancer (NSCLC) cells treated with NU7441 (0.3 μM) and radiation show significant G2/M arrest.   2016 Sep;107(9):1250-5.

    NU7441 (KU-57788)

    Low concentration of NU7441 does not seem to show double strand break (DSB) repair inhibition in X‐ray‐irradiated and carbon‐irradiated non‐small cell lung cancer (NSCLC) cells.   2016 Sep;107(9):1250-5.

    NU7441 (KU-57788)

    NU7441 (0.3 μM) causes a remarkable increase of DNA fragmentation in irradiated H1299 cells.  2016 Sep;107(9):1250-5.

    NU7441 (KU-57788)


    评论

      Home Prev Next Last page / pices

      发评论

      ×
      Your information is safe with us. * Required Fields.
      Products are for research use only;  We do not sell to patients
      Tel: 1-708-310-1919
      Fax: 1-708-557-7486
      Subscribe to our E-newsletter
      • Name*
      • *
      • E-mail*
      • *
      • instructions:
      • *
      Copyright 2020 InvivoChem LLC | All Rights Reserved
      prompt
      Do you confirm the receipt?