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Azacitidine (5-Azacytidine)
| Product Name | Azacitidine (5-Azacytidine) |
| Price: | Inquiry |
| Catalog No.: | CN00244 |
| CAS No.: | 320-67-2 |
| Molecular Formula: | C8H12N4O5 |
| Molecular Weight: | 244.2 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc(nc1=O)N |
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| Description | 5-Azacytidine is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. |
| Target | DNMT1 Nucleoside Antimetabolite/Analog Autophagy |
| In Vitro | Unmethylated CpG islands associated with a variety of genes become partially or fully methylated in tumors and can be reactivated by 5-Azacytidine[1]. 5-Azacytidine acts as weak inducers of erythroid differentiation of Friend erythroleukemia cells in the same concentration range where they affect DNA methyltransferase activity[2]. 5-Azacytidine inhibits L1210 cells with ID50 and ID90 values of 0.019 and circa 0.15 μg/mL, respectively[3]. |
| In Vivo | TdR-3H incorporation is significantly inhibited when the animals are exposed to 5-Azacitidine (100 mg/kg, i.p.) for 2 hr or longer[3]. |
| Cell Assay | Twenty mL of cells (circa 1×104 cells/mL) are pipetted into sterilized culture tubes with screw caps and incubated at 37°C overnight. The experiment is initiated by the addition of 1 mL of 5-Azacytidine (5-azaCR) or medium for a given period (from 0 to 240 min) prior to the addition of 1 mL of metabolite (or medium). Cell growth is determined twice a day for 3 days by means of a Model A Coulter counter. To determine IDSO and ID90 values, 5 mL of L1210 cells (5×103 cells/mL) are incubated with the drug at 37°C for 3 days, and cell growth is determined. |
| Animal Admin | For the in vivo experiments, leukemic mice (bearing circa 1×103 cells/animal) are given injections i.p. with 0.2 mL of 5-Azacytidine (5-azaCR) of a given concentration. Two hr later, the reaction is started by injecting 0.5 mL of labeled metabolite (TdR-3H or UR-3H, 10 /μCi/12.5 μg). After 1 hr, animals (3 mice/group) are killed by cervical fracture, and the ascites are treated with heparin, collected, pooled, and then centrifuged immediately in a Sorvall refrigerated centrifuge Model R2C-B at 800×g for 10 min (4°C). |
| Density | 2.1±0.1 g/cm3 |
| Boiling Point | 534.5±60.0 °C at 760 mmHg |
| Flash Point | 277.0±32.9 °C |
| Exact Mass | 244.080765 |
| PSA | 143.72000 |
| LogP | -1.99 |
| Vapour Pressure | 0.0±3.2 mmHg at 25°C |