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Azacitidine is used in the treatment of myelodysplastic syndrome. Cells in the presence of azacitidine incorporate it into DNA during replication and into RNA during transcription. The incorporation of azacitidine into DNA or RNA inhibits methyltransferase thereby causing demethylation in that sequence, affecting the way that cell regulation proteins are able to bind to the DNA/RNA substrate.
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Azacitidine purchased from AbMole
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Source | Exp Hematol (2013). Figure 3. Azacitidine |
| Method | Apoptosis analysis | |
| Cell Lines | MOLM-13 and SKM-1 cells | |
| Concentrations | 0.1, 0.2, 0.5, or 1 μmol/L | |
| Incubation Time | 48 h | |
| Results | Azacitidine significantly decreased viability of both leukemic cell lines as a result of an increase in apoptosis |
 |
Source | Exp Hematol (2013). Figure 1. Azacitidine |
| Method | qRT-PCR | |
| Cell Lines | MOLM-13 and SKM-1 cells | |
| Concentrations | 0.1, 0.2, 0.5, or 1 μmol/L | |
| Incubation Time | 48 h | |
| Results | As shown in Figure 1, azacitidine increased MMP9 messenger RNA (mRNA) in a dosedependent fashion in both MOLM-13 (Fig. 1A) and SKM cells (Fig. 1B). |
| Cell Experiment | |
|---|---|
| Cell lines | Leukemia L1210 cell |
| Preparation method | 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. |
| Concentrations | 0.15 μg/mL |
| Incubation time | 3 d |
| Animal Experiment | |
|---|---|
| Animal models | BDF1 mice bearing lymphoid leukemia L1210 |
| Formulation | 0.85% NaCl solution |
| Dosages | 3 mg/kg |
| Administration | i.p. |
| Molecular Weight | 244.2 |
| Formula | C8H12N4O5 |
| CAS Number | 320-67-2 |
| Solubility (25°C) | DMSO 28 mg/mL Water 22 mg/mL (ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related DNA/RNA Synthesis Products |
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| Mizoribine
Mizoribine (Bredinin) is an imidazole nucleoside and an immunosuppressive agent with an IC50 of approximately 100 μM. Mizoribine inhibits replication of SARS-CoV with IC50s of 3.5 μg/mL and 16 μg/mL for SARS-CoV Frankfurt-1 and SARS-CoV HKU39849, respectively. |
| CDDP
Cisplatin is an inorganic platinum complex that inhibits DNA synthesis by forming DNA crosslinking agents, inactivates GPXs, reduces cell GSH and induces iron death in HCT116 and A549 cells. |
| Raltitrexed
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| Carmofur
Carmofur is a pyrimidine analog that is a prodrug of 5-fluorouracil (5-FU), which inhibits DNA Synthesis and has better antiproliferative activity than 5-FU. Carmofur is an inhibitor of Acidic Ceramidase (ASAH1) and a potential lead compound for non-cancer diseases such as Krabbe disease, acute lung injury (ALI), Parkinson's disease (PD), dementia, etc. Carmofur also has antifungal and antimicrobial properties. |
| 5-Fluorouracil
5-Fluorouracil (5-FU) is a potent antitumor agent that affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. |
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