Powder: -20°C for 3 years | In solvent: -80°C for 1 year
10074-G5是一种c-Myc-Max 二聚化的抑制剂,IC50值为146 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 283 | 现货 | ||
5 mg | ¥ 497 | 现货 | ||
10 mg | ¥ 690 | 现货 | ||
25 mg | ¥ 1,150 | 现货 | ||
50 mg | ¥ 1,930 | 现货 | ||
100 mg | ¥ 3,360 | 现货 | ||
200 mg | ¥ 4,890 | 现货 | ||
500 mg | ¥ 7,580 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 547 | 现货 |
产品描述 | 10074-G5 is an inhibitor of c-Myc-Max dimerization. |
靶点活性 | c-Myc:2.8 μM(Kd) |
体外活性 | 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 [2]. |
体内活性 | 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[2]. |
细胞实验 | Daudi cells (3 × 108 cells in logarithmic growth) are incubated for 0, 1, 3, 6, or 24 h in 3 ml of complete medium containing 10 μM 10074-G5. After incubation, cells are harvested, split into two samples of 1.5 ml each, and overlaid in microcentrifuge tubes containing 0.5 ml of silicon oil. The tubes are centrifuged at 12,000 g for 4 min. After centrifugation, the top 1 ml of medium is removed and stored in cryovials at ?70°C until analysis. The remaining medium and silicon oil are carefully removed without disturbing the cell pellets. The sides of the tubes are cleaned with cotton-tipped applicators, and the cell pellets are stored at ?70°C until analysis.(Only for Reference) |
分子量 | 332.31 |
分子式 | C18H12N4O3 |
CAS No. | 413611-93-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 56 mg/mL (168.5 mM)
Ethanol: 10 mg/mL (30.09 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 3.0092 mL | 15.0462 mL | 30.0924 mL | 75.231 mL |
5 mM | 0.6018 mL | 3.0092 mL | 6.0185 mL | 15.0462 mL | |
10 mM | 0.3009 mL | 1.5046 mL | 3.0092 mL | 7.5231 mL | |
20 mM | 0.1505 mL | 0.7523 mL | 1.5046 mL | 3.7615 mL | |
DMSO | 50 mM | 0.0602 mL | 0.3009 mL | 0.6018 mL | 1.5046 mL |
100 mM | 0.0301 mL | 0.1505 mL | 0.3009 mL | 0.7523 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
10074-G5 413611-93-5 Autophagy Cell Cycle/Checkpoint c-Myc 10074G5 Inhibitor 10074 G5 10074-G-5 inhibit Myc inhibitor