1. Cell Cycle/DNA Damage
    Epigenetics
    Anti-infection
    Autophagy
  2. Nucleoside Antimetabolite/Analog
    DNA Methyltransferase
    Bacterial
    Autophagy
    Antibiotic
  3. 5-Azacytidine

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

Cat. No.: HY-10586 Purity: ≥98.0%
Handling Instructions

5-azacytidine (azacitidine; 5-azaC; ladakamycine) est un analogue nucléosidique de la cytidine qui inhibe spécifiquement la méthylation de l'ADN. 5-azacytidine est incorporée dans l'ADN pour piéger de manière covalente les ADN méthyltransférases et contribue à inverser les changements épigénétiques. 5-azacytidine induit l'autophagie cellulaire.

5-Azacytidin (Azacitidin; 5-AzaC; Ladakamycin) ist ein Nukleosidanalogon von Cytidin, das spezifisch die DNA-Methylierung hemmt. 5-Azacytidin wird in die DNA eingebaut, um DNA methyltransferases kovalent einzufangen, und trägt zur Umkehrung epigenetischer Veränderungen bei. 5-Azacytidin induziert die Zellautophagie.

5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes. 5-Azacytidine induces cell autophagy.

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

5-Azacytidine Chemical Structure

5-Azacytidine Chemical Structure

CAS No. : 320-67-2

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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 34 publication(s) in Google Scholar

Top Publications Citing Use of Products

    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.

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    Description

    5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes[1][2]. 5-Azacytidine induces cell autophagy[4].

    IC50 & Target[1]

    DNMT1

     

    Nucleoside Antimetabolite/Analog

     

    Autophagy

     

    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 ID90 values of 0.019 and circa 0.15 μg/mL, respectively[3].

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

    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].

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

    Clinical Trial
    Molecular Weight

    244.20

    Formula

    C8H12N4O5

    CAS No.
    SMILES
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    H2O : 33.33 mg/mL (136.49 mM; Need ultrasonic)

    DMSO : ≥ 31 mg/mL (126.95 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent 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.
    In Vivo:
    • 1.

      Add each solvent one by one:  PBS

      Solubility: 20 mg/mL (81.90 mM); Clear solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (8.52 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.08 mg/mL (8.52 mM); Clear solution

    • 4.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (8.52 mM); Clear solution

    *All of the co-solvents are available by MCE.
    References
    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.

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

    References

    Purity: 99.40%

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