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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 |
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| Nelarabine
Nelarabine is a novel purine antimetabolite antineoplastic agent. |
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| Capecitabine
Capecitabine is an orally-administered chemotherapeutic agent. Capecitabine is a precursor, that is enzymatically converted to 5-fluorouracil in the tumor, where it inhibits DNA synthesis and slows growth of tumor tissue. Capecitabine may inhibit cytochrome CYP2C9 enzyme, and therefore increase levels of substrates such as phenytoin and other substrates of CYP2C9. |
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