首页 产品中心
  • 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
    分享:
    货号-规格 货期 价格 数量
    abs813455-5mg 1-2周 ¥679.00
    - +
    abs813455-10mg 1-2周 ¥938.00
    - +
    abs813455-25mg 1-2周 ¥1504.00
    - +
    abs813455-50mg 1-2周 ¥2535.00
    - +
    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);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    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:
    温馨提示:本产品仅作科研实验使用,不支持临床等研究
    • 实验方法 实验条件
      0 张,还能上传 8 提交
          提示: 尊敬的客户您好,如果您对我们的产品有什么疑问或想要了解的,可以点击“我要咨询”按钮填写您的疑问。
          提交不成功?请联系info@absin.cn。
          我要咨询

      促销资讯 更多

        订购信息
        您可以从我们的授权经销商处购买absin产品或获得技术支持。若要查看您所在地区的经销商,请从以下的下拉列表中选择。
        GO
        • 0