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    NU1025
    NU1025

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0308
    CAS #: 90417-38-2Purity ≥98%

    Description: NU1025 is a novel, potent and selective inhibitor of poly(ADP-ribose) polymerase (PARP) inhibitor with potential anticancer activity. It shows potent antiproliferative activity against various cancer cells and high in vivo antitumor efficacy as well. NU1025 ia able to potentiate the cytotoxicity of a diverse set of anti-cancer agents in L1210 cells.  

    References: Life Sci. 2006 Nov 10;79(24):2293-302.

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    Molecular Weight (MW)176.17
    FormulaC9H8N2O2
    CAS No.90417-38-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 35 mg/mL (198.7 mM)   
    Water: <1 mg/mL
    Ethanol: 6 mg/mL warmed (34.1 mM)
    Solubility (In vivo)40% PEG 400+saline: 18mg/mL 
    Synonyms

    Synonym: NU 1025; NU1025; NU-1025.

    Chemical Name: 8-Hydroxy-2-methyl-4(3H)-quinazolinone

    InChi Key: YJDAOHJWLUNFLX-UHFFFAOYSA-N

    InChi Code: InChI=1S/C9H8N2O2/c1-5-10-8-6(9(13)11-5)3-2-4-7(8)12/h2-4,12H,1H3,(H,10,11,13)

    SMILES Code: O=C1NC(C)=NC2=C1C=CC=C2O


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    In Vitro

    In vitro activity: NU1025 (0.2 mM) treatment attenuates H2O2 induced cytotoxicity. NU1025 per se does not have any effect on cell viability. NU1025 pretreatment significantly increases cell viability (82.59 ?4.67%) in SIN-1 (0.8 mM) exposed cells. NU1025 has no detectable effect on the proliferation of D54 and U251 cells. Treatment with NU1025 markedly inhibits the enhanced activation of PARP-1 induced by TPT and RT treatment. No DNA strand breakage is detected following exposure to 200 µM NU1025 alone


    Kinase Assay: Cells are suspended in hypotonic buffer (9 mM HEPES, pH 7.8, 4.5% (v/v) dextran, 4.5 mM MgCl2 and 5 mM DTT) at 1.5 × 107/mL on ice for 30 min, then 9 vol of isotonic buffer (40 mM HEPES, pH 7.8, 130 mM KCl, 4% (v/v) dextran, 2 mM EGTA, 2.3 mM MgCl2, 225 mM sucrose and 2.5 mM DTT) is added. The reaction is started by adding 300 µL cells to 100 µL 300 µM NAD+ containing [32P]-NAD+, and terminated by the addition of 2 mL ice-cold 10% (w/v) TCA +10% (w/v) sodium pyrophosphate. After 30 min on ice the precipitated 32P-labelled ADP-ribose polymers are filtered, washed five times with 1% (v/v) TCA, 1% (v/v) sodium pyrophosphate, dried and counted.


    Cell Assay: Cells (D54 and U251 cells) are seeded in 96-well plates at a density of 2,500 cells/well and treated with the indicated doses of NU1025. Adherent cells are irradiated in medium with 250 kVp X-rays (dose rate 0.5 Gy/min). Untreated cells are used as a control. Following an up to 5 day incubation, cell proliferation is assessed by MTT assay.

    In VivoTreatment with NU1025 (1 and 3 mg/kg) reduces the infarction to 25% and 45% versus vehicle treated rats, respectively. NU1025 (1 and 3 mg/kg) treatment significantly reduces edema volume. NU1025 also produces significant improvement in neurological deficits.
    Animal modelMale Sprague Dawley rats
    Formulation & DosageDissolved in 40% PEG 400 in saline; 3 mg/kg;  i.p. injection
    References

    Life Sci. 2006 Nov 10;79(24):2293-302.


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

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