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Azacitidine

Cat. No. M2291
Azacitidine Structure
Synonym:

5-azacytidine, Mylosar, Ladakamycin

Size Price Availability Quantity
200mg USD 120 In stock
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Quality Control
Biological Activity

Azacitidine (Vidaza) 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.

Customer Product Validations & Biological Datas
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).
Protocol
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 244.2
Formula C8H12N4O5
CAS Number 320-67-2
Purity 99.39%
Solubility DMSO 30 mg/mL
Storage at -20°C
References

Pharmacokinetics of different formulations of oral azacitidine (CC-486) and the effect of food and modified gastric pH on pharmacokinetics in subjects with hematologic malignancies.
Laille E, et al. J Clin Pharmacol. 2014 Jun;54(6):630-9. PMID: 24374798.

Comparative analysis between azacitidine and decitabine for the treatment of myelodysplastic syndromes.
Lee YG, et al. Br J Haematol. 2013 May;161(3):339-47. PMID: 23432512.

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Keywords: Azacitidine, 5-azacytidine, Mylosar, Ladakamycin supplier, DNA/RNA Synthesis, inhibitors

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