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5-Azacytidine (Ladakamycin) 是一种胞苷核苷类似物,一种 DNA 甲基化抑制剂,具有特异性。5-Azacytidine 通过降低 DNA 甲基化水平调节基因表达。5-Azacytidine 可以诱导细胞自噬,具有抗肿瘤活性。
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5-Azacytidine (Ladakamycin) 是一种胞苷核苷类似物,一种 DNA 甲基化抑制剂,具有特异性。5-Azacytidine 通过降低 DNA 甲基化水平调节基因表达。5-Azacytidine 可以诱导细胞自噬,具有抗肿瘤活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
50 mg | ¥ 184 | 现货 | |
100 mg | ¥ 287 | 现货 | |
200 mg | ¥ 523 | 现货 | |
500 mg | ¥ 988 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 376 | 现货 |
产品描述 | 5-Azacytidine (Ladakamycin) is a cytidine nucleoside analog, a DNA methylation inhibitor with specificity. 5-Azacytidine regulates gene expression by decreasing the level of DNA methylation. 5-Azacytidine induces autophagy and has antitumor activity. |
体外活性 | 方法:人胰腺癌细胞 PANC-1、Capan-2、PL45 和 SU.86-86 用 5-Azacytidine (2.5-30 μM) 处理 1-5 天,使用 MTT 检测细胞活力。 结果:5-Azacytidine 显示出明显的剂量-反应效应。Capan-2 和 PANC-1 细胞对 5-Azacytidine 的耐药性最强,暴露 48 h 后 IC50 分别为 71.3 和 45.6 μM。SU.86.86 细胞对 5-Azacytidine 更敏感,48 h 的 IC50 为 19.2 μM。[1] 方法:人多发性骨髓瘤细胞 MM.1S 用 5-Azacytidine (1.25-5 μM) 处理 16-72 h,使用 Flow Cytometry 方法检测细胞凋亡情况。 结果:5-Azacytidine 治疗以剂量依赖的方式增加了 24 h 后 Annexin V 阳性的细胞比例,在 72 h 达到峰值。5-Azacytidine 诱导细胞凋亡。[2] |
体内活性 | 方法:为检测体内抗肿瘤活性,将 5-Azacytidine (3 mg/kg) 腹腔注射给携带人胰腺癌肿瘤 PANC-1 的 athymic nude 小鼠,每周六次,持续四周。 结果:肿瘤在注射 5-Azacytidine 后明显变小,肿瘤进展受到显著抑制。[1] 方法:为研究在白血病中的作用,将 5-Azacytidine (5 mg/kg) 腹腔注射给用 C1498 细胞构建白血病模型的 C57BL/6 小鼠,每天一次,持续三天。 结果:5-Azacytidine 治疗在白血病小鼠中重新建立了免疫相关转录物的表达,抑制了白血病负荷并延长了生存期。5-Azacytidine 治疗的效果是短暂的,对免疫微环境的分析揭示了耐药性的可能机制,例如免疫检查点蛋白表达的同时增加。[3] |
激酶实验 | A crude cell-free extract is isolated from LI 210 cells in culture by suspension of the cells in a given volume of 0.05mol/LTris-HCl buffer, pH 7.4, and sonic extraction with a Biosonik at 70% maximal output for 30 sec. The supernatant is collected after centrifugation at 105,000 × g for 60 min (4°C) in a Model L Spinco ultracentrifuge. The final protein concentration of the cell-free extracts is approximately 3 mg/mL. The extracts are used as the source of enzymes. Ribonucleotide reductase activity is measured. A unit of enzyme is defined as the amount that catalyzed dCMP synthesis at a rate of 1 mμmole/hr. The assay systems for the measurement of pyrimidine nucleoside (CR) and deoxynucleoside (TdR, CdR) kinases are essentially those described by Chu and Fischer. However, reactions are terminated by heating for 2 min in a boiling water bath, and the phosphorylated derivatives are isolated according to the method of Bach. Fifty-jul aliquots are applied to 1-inch discs of diethylaminoethyl paper, which are then placed in counting vials and eluted with 0.5 mL of 0.5 mol/LPCA. After 1 hr, 12 mL of Diotol are added, and the radioactivity is determined. |
细胞实验 | 5 mL of L1210 cells (5 × 103 cells/mL) are incubated with Azacitidine at 37 ℃ for 3 days. Cell number is determined twice a day for 3 days by means of a Model A Coulter counter.(Only for Reference) |
别名 | 5-氮杂胞苷, 阿托胞苷, Azacitidine, NSC 102816, Mylosar, Ladakamycin, 5-AzaC |
分子量 | 244.2 |
分子式 | C8H12N4O5 |
CAS No. | 320-67-2 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||
溶解度信息 | DMSO: 100 mg/mL (409.5 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) 5% DMSO+40% PEG300+5% Tween 80+50% Saline: 1 mg/mL (4.1 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. 5% DMSO+95% Saline: 1 mg/mL (4.1 mM), Working solution is recommended to be prepared and used immediately. | ||||||||||
溶液配制表 | |||||||||||
5% DMSO+40% PEG300+5% Tween 80+50% Saline/5% DMSO+95% Saline/DMSO
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