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  • 10074-G5
  • N-2-联苯基-7-硝基-2,1,3-苯并恶二唑-4-胺
  • 货号: abs813455
    CAS号: 413611-93-5
    分子式: C18H12N4O3
    分子量: 332.31
    产品说明书
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    货号-规格 货期 价格 数量
    abs813455-5mg 1-2周 ¥647.00
    - +
    abs813455-10mg 1-2周 ¥893.00
    - +
    abs813455-25mg 1-2周 ¥1432.00
    - +
    abs813455-50mg 1-2周 ¥2414.00
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    大包装询价
    产品描述
    描述

    10074-G5 is an inhibitor of c-Myc-Max dimerization (IC50 =146 μM) that operates by binding and stabilizing c-Myc in its monomeric form. 10074-G5 inhibits c-Myc/Max heterodimer formation and its transcriptional activity. 10074-G5 is most efficient in inducing neuronal differentiation and lipid accumulation in MYCN-amplified neuroblastoma cells.

    纯度
    >97%
    储存/保存方法
    store at -20℃ for one year(Powder);
    in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.
    基本信息
    别名
    N-2-联苯基-7-硝基-2,1,3-苯并恶二唑-4-胺
    外观
    red powder
    可溶性/溶解性
    Ethanol :10 mg/mL (30.09 mM)

    DMSO :56 mg/mL (168.5 mM)
    生物活性
    靶点
    c-Myc
    In vitro(体外研究)
    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 inhibits the growth of Daudi Burkitt's lymphoma cells and disrupts c-Myc/Max dimerization. Daudi cells accumulates 10074-G5, and the highest intracellular concentration is observed at 6 h. 10074-G5 inhibits c-Myc/Max dimerization in Daudi cells by approximately 75% at 4 h, and this inhibition is maintained through 24 h of incubation. Total c-Myc protein expression also decreases, and after 24 h exposure to 10 μM 10074-G5, c-Myc protein expression decreases approximately 40% compared with vehicle-treated control. 10074-G5 is cytotoxic in vitro against Daudi and HL-60 cells, which overexpress c-Myc .
    In vivo(体内研究)
    The 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.
    参考文献
    参考文献
    Discovery of Methyl 4'-Methyl-5-(7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)-[1,1'-biphenyl]-3-carboxylate, an Improved Small-Molecule Inhibitor of c-Myc-Max Dimerization.
    Chauhan J, et al. ChemMedChem. 2014 Jun 27. PMID: 24976143.
    Targeting of the MYCN Protein with Small Molecule c-MYC Inhibitors.
    Müller I, et al. PloS one. 2014 May 23;9(5):e97285. PMID: 24859015.
    In vitro cytotoxicity and in vivo efficacy, pharmacokinetics, and metabolism of 10074-G5, a novel small-molecule inhibitor of c-Myc/Max dimerization.
    Clausen DM, et al. Journal of Pharmacology and Experimental Therapeutics. 2010 Dec;335(3):715-727. PMID: 20801893.
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