| 中文名称: | 3-去氮腺嘌呤A | ||||
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| 英文名称: | 3-Deazaneplanocin A | ||||
| 别名: | DZNep; 3-Deazaneplanocin | ||||
| CAS No: | 102052-95-9 | 分子式: | C12H14N4O3 | 分子量: | 262.26 |
| CAS No: | 102052-95-9 | ||||
| 分子式: | C12H14N4O3 | ||||
| 分子量: | 262.26 | ||||
基本信息
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产品编号：D10839 |
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产品名称：3-Deazaneplanocin A |
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CAS: |
102052-95-9 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
六个月 |
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分子量： |
262.26 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
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Ethanol |
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Water |
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体内（现配现用） |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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生物活性
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产品描述 |
一种有效的组蛋白甲基转移酶 (histone methyltransferase，EZH2) 抑制剂。3-Deazaneplanocin A 是一种有效的 S-腺苷同型半胱氨酸水解酶 (AHCY) 抑制剂。 |
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靶点/IC50 |
EZH2 |
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体外研究 |
3-Deazaneplanocin A is a potent histone methyltransferase EZH2 inhibitor. Treatment of OCI-AML3 cells with 3-Deazaneplanocin A (1.0μM) results in a significant increase in accumulation of cells in the G0/G1 phase (58.5%) with a concomitant decrease in the number of cells in S phase (35.2%) and G2/M phases (6.3%) of the cell cycle (P<0.05).Treatment with 3-Deazaneplanocin A (200nM to 2.0μM) for 48 hours,dose dependently,inhibits colony growth of OCI-AML3 and HL-60 cells.3-Deazaneplanocin A reduces the expression of EZH2, especially after 72 hours (e.g.48%,32% and 36% reduction of EZH2 in PANC-1,MIA-PaCa-2 and LPc006 cells,respectively).3-Deazaneplanocin A shows minimal growth inhibition in PANC-1 cells.More than 50% of these cells are still growing after exposure at the highest concentration (20μM).MIA-PaCa-2 and LPc006 cells are much more sensitive,with IC0 values of 1±0.3 and 0.1±0.03μM,respectively.3-Deazaneplanocin A causes dose-dependent inhibition of cell proliferation of NSCLC cell lines, and the IC0 values range from 0.08 to 0.24μM. |
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体内研究 |
The survival of NOD/SCID mice with acute myeloid leukemia (AML) due to HL-60 cells is significantly higher,if treated with 3-Deazaneplanocin A and Panobinostat (PS) compare to treatment with PS,3-Deazaneplanocin A, or vehicle alone (P<0.05).Median survival is as follows:control,36 days;PS,42 days;3-Deazaneplanocin A,43 days;and 3-Deazaneplanocin A plus PS,52 days. There is a progressive increase in weight of rats treated with physiological saline in a time-dependent manner (the mean growth rate=3.19% per day).Administration of 20mg/kg 3-Deazaneplanocin A not only markedly reduces the relative weight of the rats compare to the initial weight (−2.0%,−4.9% and −1.2%) in the first three days post-treatment, but also suppresses the weight growth rate to 2.6% per day from the fourth day onwards post-dose. |
推荐实验方法(仅供参考)
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细胞实验: |
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AML HL-60 cells are obtained and maintained.OCI-AML-3 cells are cultured in α minimum essential medium with 10% fetal bovine serum,1% penicillin/streptomycin,and 1% nonessential amino acids.To analyze synergism between 3-Deazaneplanocin A and PS in inducing apoptosis,cells are treated with 3-Deazaneplanocin A (100-750nM) and PS (5-20nM) at a constant ratio for 48 hours.The percentage of apoptotic cells is determined by flow cytometry.The combination index (CI) for each drug combination is obtained by median dose effect of Chou and Talalay,using the CI equation within the commercially available software Calcusyn. |
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动物实验: |
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Rats Male wistar rats are used.The acute toxicity study is carried out to determine the NOAEL of 3-Deazaneplanocin A in rats.In total,20 rats are divided into 4 groups of five each.Three groups are intravenously administered 20,15,10mg/kg body weight (BW) 3-Deazaneplanocin A solution by the tail vein.The remaining group is given physiological saline (0.9% NaCl saline) as the control group.Then,the NOAEL of free 3-Deazaneplanocin A is determined,depending on the following endpoint parameters obtained. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
