- N-2-联苯基-7-硝基-2,1,3-苯并恶二唑-4-胺
货号： abs813455
| 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）；
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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Certificate of Analysis(COA)
