2. Stem Cell/Wnt Cell Cycle/DNA Damage Epigenetics Anti-infection Autophagy
  3. Organoid Nucleoside Antimetabolite/Analog DNA Methyltransferase Bacterial Autophagy Antibiotic
  4. 5-Azacytidine

5-アザシチジン  (Synonyms: アザシチジン; Azacitidine; 5-Azacytidine; Ladakamycin; AZA; 5-Aza)

製品番号: HY-10586 純度: 98.03%
COA 取扱説明書 Technical Support

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.

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CAS 番号 : 320-67-2

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 在庫あり
Solution
10 mM * 1 mL in DMSO USD 66 在庫あり
Solid
100 mg $60 在庫あり
200 mg $72 在庫あり
500 mg $119 在庫あり
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5 g   お問い合わせ  

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カスタマーレビュー

Based on 128 publication(s) in Google Scholar

Other Forms of 5-Azacytidine:

5-アザシチジン 関連抗体

Top Publications Citing Use of Products

顧客検証

RT-PCR
WB

    5-Azacytidine purchased from MedChemExpress. Usage Cited in: Nature. 2025 Jan;637(8045):461-469.  [Abstract]

    5-Azacytidine (5 μM, 5 days) reverses FBP1 promoter methylation and restores FBP1 protein levels in SK-HEP-1 and HepG2 cells.

    5-Azacytidine purchased from MedChemExpress. Usage Cited in: Drug Resist Updat. 2024 Jul 22:76:101120.  [Abstract]

    Western blot were conducted to examine the BCL7A levels in AML cells treated with different concentrations of 5-AzaC (5-Azacytidine) (0, 20, 40 μM).

    5-Azacytidine purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2023 Dec 4;22(1):195.  [Abstract]

    5-Azacytidine (5µM; 72 h) increases the expression of LIG1 in GEM-resistant cells.

    5-Azacytidine purchased from MedChemExpress. Usage Cited in: Int J Biol Macromol. 2022 Dec 31;223(Pt A):916-930.

    5-azacytidine (5-AzaC; 5 μM; 1, 2, 3 days) results in an increase in the expression of MYOD1 and MYOG during myoblast differentiation.

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

    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.

    DNA Methyltransferase アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    DNA Methyltransferase DNMT1 DNMT3 MGMT

    Antibiotic アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    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

     

    Cellular Effect
    Cell Line Type Value Description References
    5637 IC50
    1.73 μM
    Compound: 5-Aza-cytidine
    Antiproliferative activity against human 5637 cells after 96 hrs by crystal violet assay
    Antiproliferative activity against human 5637 cells after 96 hrs by crystal violet assay
    		[PMID: 18434163]
    A-427 IC50
    0.63 μM
    Compound: 5-Aza-cytidine
    Antiproliferative activity against human A427 cells after 96 hrs by crystal violet assay
    Antiproliferative activity against human A427 cells after 96 hrs by crystal violet assay
    		[PMID: 18434163]
    HEK293 IC50
    > 500 μM
    Compound: azacitidine
    Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
    Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
    		[PMID: 23241029]
    HT-29 IC50
    3800 nM
    Compound: 5-azacytidine
    Antiproliferative activity against human HT-29 cells after 96 hrs by MTT assay
    Antiproliferative activity against human HT-29 cells after 96 hrs by MTT assay
    		[PMID: 2778449]
    KB IC50
    0.23 μg/mL
    Compound: 80
    Growth inhibition of human KB cells
    Growth inhibition of human KB cells
    		[PMID: 29135244]
    L1210 IC50
    4.09 x 10-7 M
    Compound: AZC
    Compound was tested for its inhibitory activity against L1210 lymphoid leukemia
    Compound was tested for its inhibitory activity against L1210 lymphoid leukemia
    		[PMID: 3806615]
    MCF7 IC50
    6.78 μM
    Compound: 5-Aza-cytidine
    Antiproliferative activity against human MCF7 cells after 96 hrs by crystal violet assay
    Antiproliferative activity against human MCF7 cells after 96 hrs by crystal violet assay
    		[PMID: 18434163]
    P388 IC50
    5000 nM
    Compound: 5-azacytidine
    Antiproliferative activity against mouse P388 cells after 48 hrs by MTT assay
    Antiproliferative activity against mouse P388 cells after 48 hrs by MTT assay
    		[PMID: 2778449]
    体外実験

    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].

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

    5-アザシチジン 関連抗体
    体内実験

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    244.20

    分子式

    C8H12N4O5
    CAS 番号
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    OC[C@@H]1[C@@H](O)[C@@H](O)[C@H](N2C(N=C(N)N=C2)=O)O1
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 250 mg/mL (1023.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 25 mg/mL (102.38 mM; ultrasonic and warming and heat to 60°C)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

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    体積 （終了）

    V2

    体内:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

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

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    純度とドキュメンテーション

    純度: 99.91%

    COA (253 KB) LCMS (93 KB)

    取扱説明書 (2659 KB)
    参考文献
    キナーゼ実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    細胞実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 4.0950 mL 20.4750 mL 40.9500 mL 102.3751 mL
    5 mM 0.8190 mL 4.0950 mL 8.1900 mL 20.4750 mL
    10 mM 0.4095 mL 2.0475 mL 4.0950 mL 10.2375 mL
    15 mM 0.2730 mL 1.3650 mL 2.7300 mL 6.8250 mL
    20 mM 0.2048 mL 1.0238 mL 2.0475 mL 5.1188 mL
    25 mM 0.1638 mL 0.8190 mL 1.6380 mL 4.0950 mL
    30 mM 0.1365 mL 0.6825 mL 1.3650 mL 3.4125 mL
    40 mM 0.1024 mL 0.5119 mL 1.0238 mL 2.5594 mL
    50 mM 0.0819 mL 0.4095 mL 0.8190 mL 2.0475 mL
    60 mM 0.0683 mL 0.3413 mL 0.6825 mL 1.7063 mL
    80 mM 0.0512 mL 0.2559 mL 0.5119 mL 1.2797 mL
    100 mM 0.0410 mL 0.2048 mL 0.4095 mL 1.0238 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    5-Azacytidine Related Classifications

    • Molarity Calculator

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    5-Azacytidine320-67-2Azacitidine 5-AzaC LadakamycinOrganoidNucleoside Antimetabolite/AnalogDNA MethyltransferaseBacterialAutophagyAntibioticDNMTsDNA MTasesInhibitorinhibitorinhibit

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    製品番号:
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