5-Azacytidine是特异性 DNA 甲基化抑制剂，是胞苷核苷类似物。它诱导细胞自噬。通过DNA 结合共价捕获 DNA甲基转移酶，对逆转表观遗传变化有益。

Azacitidine, a pyrimidine nucleoside analogue of cytidine, blocks DNA methylation with antineoplastic activity.

在携带有L11210腹水肿瘤细胞的白血病BDF1小鼠中,腹腔注射Azacitidine（3 mg / kg）,抑制多核苷酸合成,提高小鼠存活时间.

在正常的真核细胞和癌细胞中,Azacitidine可激活核苷三磷酸,抑制DNA、RNA和蛋白合成,最终导致细胞死亡。在C3H10T1/2细胞中,Azacitidine 诱导细胞分化和肌管形成。在 L1210细胞中（IC50=0.019 μg/mL）,Azacitidine 抑制细胞生长。

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.

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)

320-67-2

C8H12N4O5

244.207

5-AzaC;Ladakamycin;Mylosar;NSC 102816;5-氮杂胞苷;阿托胞苷;Azacitidine

DMSO:24.4 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years