Powder: -20°C for 3 years | In solvent: -80°C for 1 year
3-deazaneplanocin A HCl 是组蛋白甲基转移酶 (EZH2) 和 S-腺苷同型半胱氨酸水解酶 (AHCY) 抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 747 | 现货 | ||
5 mg | ¥ 2,570 | 现货 | ||
10 mg | ¥ 3,970 | 现货 | ||
25 mg | ¥ 7,260 | 现货 | ||
50 mg | ¥ 9,790 | 现货 | ||
100 mg | ¥ 13,200 | 现货 |
产品描述 | 3-deazaneplanocin A HCl is both an S-adenosyl-l-homocysteine hydrolase inhibitor and an enhancer of zeste homolog 2(EZH2) inhibitor. |
体外活性 | EZH2 expression was detected by quantitative PCR in 15 PDAC cells, including seven primary cell cultures, showing that expression values correlated with their originator tumors (Spearman R(2) = 0.89, P = 0.01). EZH2 expression in cancer cells was significantly higher than in normal ductal pancreatic cells and fibroblasts. The 3-deazaneplanocin A HCl(5 μmol/L, 72-hour exposure) modulated EZH2 and H3K27me3 protein expression and synergistically enhanced the antiproliferative activity of gemcitabine, with combination index values of 0.2 (PANC-1), 0.3 (MIA-PaCa-2), and 0.7 (LPC006). The drug combination reduced the percentages of cells in G(2)-M phase (e.g., from 27% to 19% in PANC-1, P < 0.05) and significantly increased apoptosis compared with gemcitabine alone. Moreover, 3-deazaneplanocin A HCl enhanced the mRNA and protein expression of the nucleoside transporters hENT1/hCNT1. 3-deazaneplanocin A HCl decreased cell migration, which was additionally reduced by 3-deazaneplanocin A HCl/gemcitabine combination (-20% in LPC006, after 8-hour exposure, P < 0.05) and associated with increased E-cadherin mRNA and protein expression. Furthermore, 3-deazaneplanocin A HCl and 3-deazaneplanocin A HCl/gemcitabine combination significantly reduced the volume of PDAC spheroids growing in CSC-selective medium and decreased the proportion of CD133+ cells[2]. |
体内活性 | The survival of NOD/SCID mice with AML due to HL-60 cells was significantly higher, if treated with 3-deazaneplanocin A HCl and PS compared to treatment with PS, 3-deazaneplanocin A HCl, or vehicle alone (P < .05). Cotreatment with 3-deazaneplanocin A HCl and PS also did not increase the weight loss in the mice. Median survival was as follows: control, 36 days; PS, 42 days; 3-deazaneplanocin A HCl, 43 days; and 3-deazaneplanocin A HCl plus PS, 52 days.Compared with treatment with each agent alone, combined treatment with 3-deazaneplanocin A HCl and PS improved survival of NOD/SCID mice with leukemia caused by the AML HL-60 cells[3]. |
分子量 | 298.73 |
分子式 | C12H15ClN4O3 |
CAS No. | 120964-45-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 50 mg/mL (167.38 mM), Sonication is recommended.
DMSO: 50 mg/mL (167.38 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O / DMSO | 1 mM | 3.3475 mL | 16.7375 mL | 33.475 mL | 83.6876 mL |
5 mM | 0.6695 mL | 3.3475 mL | 6.695 mL | 16.7375 mL | |
10 mM | 0.3348 mL | 1.6738 mL | 3.3475 mL | 8.3688 mL | |
20 mM | 0.1674 mL | 0.8369 mL | 1.6738 mL | 4.1844 mL | |
50 mM | 0.067 mL | 0.3348 mL | 0.6695 mL | 1.6738 mL | |
100 mM | 0.0335 mL | 0.1674 mL | 0.3348 mL | 0.8369 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。
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