1. Cell Cycle/DNA Damage
    Autophagy
    Epigenetics
  2. Nucleoside Antimetabolite/Analog
    Autophagy
    DNA Methyltransferase

5-Azacytidine (Synonyms: Ladakamycin; 5-AzaC; Azacitidine)

Cat. No.: HY-10586 Purity: 99.97%
Handling Instructions

5-Azacytidine is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases.

For research use only. We do not sell to patients.

5-Azacytidine Chemical Structure

5-Azacytidine Chemical Structure

CAS No. : 320-67-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
100 mg USD 60 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg USD 72 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
500 mg USD 119 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
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    5-Azacytidine purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129.

    The effects of treatment with the indicated epigenetic inhibitors on cleaved PARP (Clv-PARP) expression in both PC9/ER and HCC827/ER cells. β-actin is used as a loading control.

    5-Azacytidine purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129.

    H3K9Me2, PTEN, p-AKT, and AKT expression levels are measured in PC9/ER xenograft tumor tissues. β-actin is used as a loading control.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    5-Azacytidine is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases.

    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 ID50 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].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 4.0950 mL 20.4750 mL 40.9500 mL
    5 mM 0.8190 mL 4.0950 mL 8.1900 mL
    10 mM 0.4095 mL 2.0475 mL 4.0950 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [3]

    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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [3]

    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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    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). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    244.2

    Formula

    C₈H₁₂N₄O₅

    CAS No.

    320-67-2

    SMILES

    OC[[email protected]]1O[[email protected]@H](N2C(N=C(N)N=C2)=O)[[email protected]](O)[[email protected]@H]1O

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 31 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.97%

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    Product Name:
    5-Azacytidine
    Cat. No.:
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