Size : 100mg
Phone : +1 850 650 7790
Synonyms: NSC 102816, Mylosar, Ladakamycin, Azacitidine, 5-AzaC
| Description | 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. |
| Targets & IC50 | KYSE70 cells viability:1.59 ± 1.93 μM, MCF-7 cells viability:6.78 ± 5.21 μM, 5637 cells viability:1.73 ± 1.20 μM, A427 cells viability:0.63 ± 0.05 μM |
| In vitro | In leukemic BDF1 mice bearing L1210 ascitic tumor cells, intraperitoneal administration of Azacitidine (3 mg/kg) inhibits polynucleotide synthesis and prolongs survival time. |
| In vivo | In both regular eukaryotic cells and cancer cells, Azacitidine activates nucleoside triphosphates and inhibits the synthesis of DNA, RNA, and proteins, ultimately leading to cell death. Azacitidine induces cell differentiation and myotube formation in C3H10T1/2 cells. Additionally, Azacitidine suppresses cell growth in L1210 cells (IC50=0.019 μg/mL). |
| Synonyms | NSC 102816, Mylosar, Ladakamycin, Azacitidine, 5-AzaC |
| Kinase Assay | 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. |
| Cell Research | 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) |
| Molecular Weight | 244.2 |
| Formula | C8H12N4O5 |
| Cas No. | 320-67-2 |
| Smiles | O[C@H]1[C@@H](O[C@H](CO)[C@H]1O)N2C(=O)N=C(N)N=C2 |
| Relative Density. | 2.08 g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 262.5 mg/mL (1074.94 mM), Sonication is recommended.  H2O: 10 mg/mL (40.95 mM), Sonication and heating are recommended. | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | PBS: 10 mg/mL (40.95 mM), Sonication and heating are recommended. 5% DMSO+40% PEG300+5% Tween 80+50% Saline: 1 mg/mL (4.1 mM), Solution. Please add the 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. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | |||||||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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