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    10074-G5
    10074-G5

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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 #: V2724
    CAS #: 413611-93-5Purity ≥98%

    Description: 10074-G5 is a potent inhibitor of c-Myc-Max dimerization and interaction with an IC50 of 146 μM and with anticancer activities. 10074-G5 binds to and distorts the bHLH-ZIP domain of c-Myc, thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity. In vitro, 10074-G5 inhibited the growth of Daudi Burkitt's lymphoma cells and disrupted c-Myc/Max dimerization. 10074-G5 had no effect on the growth of Daudi xenografts in C.B-17 SCID mice that were treated with 20 mg/kg 10074-G5 intravenously for 5 consecutive days. Inhibition of c-Myc/Max dimerization in Daudi xenografts was not seen 2 or 24 h after treatment. 

    References: Bioorg Med Chem Lett. 2013 Jan 1;23(1):370-4; J Pharmacol Exp Ther. 2010 Dec;335(3):715-27.


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    Molecular Weight (MW)332.31
    FormulaC18H12N4O3
    CAS No.413611-93-5
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 60 mg/mL (180.5 mM)
    Water: <1 mg/mL
    Ethanol: 10 mg/mL (30.0 mM)
    SMILES O=[N+](C1=CC=C(NC2=CC=CC=C2C3=CC=CC=C3)C4=CNON41)[O-]
    Synonyms 10074-G5; 10074G5; 10074 G5 


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    In Vitro

    In vitro activity: 10074-G5 inhibits the growth of Daudi Burkitt's lymphoma cells and disruptes c-Myc/Max dimerization. The IC50 values against Daudi and HL-60 cells are 15.6 and 13.5 μM, respectively. 10074-G5 binds the Myc peptide Myc353-437 with a Kd value of 2.8 μM in the region Arg363-Ile381. 10074-G5 binds in a cavity that is created by a kink (Asp379-Ile381) in the N-terminus of an induced helical domain (Leu370–Arg378.


    Kinase Assay: 10074-G5 is a potent inhibitor of c-Myc-Max dimerization and interaction with an IC50 of 146 μM and with anticancer activities. 10074-G5 binds to and distorts the bHLH-ZIP domain of c-Myc, thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity.  


    Cell Assay: 10074-G5 is dissolved in DMSO and diluted with culture medium. Daudi cells or HL-60 cells in logarithmic growth are treated with 10074-G5 (1-100 μM). After 72 h, 50 μL of 1 mg/mL MTT is added to each well and incubated for 4 h. At the end of the incubation, medium containing drug and MTT is removed from each well, and 100 μl of DMSO is added, followed by shaking for 5 min. The absorbance at 570 nm is read.

    In VivoThe plasma half-life of 10074-G5 in mice treated with 20 mg/kg i.v. is 37 min, and peak plasma concentration is 58 μM, which is 10-fold higher than peak tumor concentration. The lack of antitumor activity probably is caused by the rapid metabolism of 10074-G5 to inactive metabolites, resulting in tumor concentrations of 10074-G5 insufficient to inhibit c-Myc/Max dimerization. Plasma 10074-G5 peak concentration (Cmax) of 58.5 ± 2.7 nmol/ml is observed at 5 min after intravenous administration of 20 mg/kg to mice bearing Daudi xenografts, 10074-G5 concentration in plasma declines rapidly. Except for lung, liver, and fat, tissue concentrations of 10074-G5 are lower than those of plasma at all time points.
    Animal modelSpecific-pathogen-free, female C.B-17 SCID mice. 
    Formulation & DosageDissolved in Cremophor EL/ethanol/saline (1:1:8, v/v/v); 20 mg/kg; i.v. injection.
    ReferencesBioorg Med Chem Lett. 2013 Jan 1;23(1):370-4; J Pharmacol Exp Ther. 2010 Dec;335(3):715-27.


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

    10074-G5

    In vitro analysis of 10074-G5 against Daudi Burkitt's lymphoma cells. J Pharmacol Exp Ther. 2010 Dec;335(3):715-27.
     

    10074-G5

    Efficacy study of 10074-G5 in mice bearing Daudi tumor xenografts. J Pharmacol Exp Ther. 2010 Dec;335(3):715-27.
     

    10074-G5

    Coimmunoprecipitation and immunoblot analysis of c-Myc and Max protein expression in Daudi xenografts from mice treated for 5 days with 20 mg/kg i.v. 10074-G5. J Pharmacol Exp Ther. 2010 Dec;335(3):715-27.


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