Azacitidine (5-Azacytidine)

Catalog No.S1782 Batch:S178209

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Technical Data

Formula

C8H12N4O5
Molecular Weight 244.2 CAS No. 320-67-2
Solubility (25°C)* In vitro DMSO 49 mg/mL (200.65 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 30%PEG300 65%ddH2O
10.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 300 μL of PEG 300, mix evenly to clarify it; then continue to add 650 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486,NSC 102816) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy.
Targets
DNA methyltransferase [1]
(Cell-free assay)
In vitro

Azacitidine is widely used to demonstrate the correlation between loss of methylation in specifc gene regions and activation of the associated genes. After incorporation into DNA, Azacitidine inhibits DNA methyltransferase noncompetitively, causing a block in cytosine methylation in newly replicated DNA but not in resting, nondividing cells. [1] Azacitidine induces differentiation of Friend Erythroleukemia Cell C3H10T1/2 with myotube formation. [2] Azacitidine can be activated to the nucleoside triphosphate and incorporate into both DNA and RNA, leading to inhibition of DNA, RNA and protein synthesis in normal eukaryotic cells and in cancer cell lines, which could finally leads to cell death. Azacitidine also inhibits the incorporation of purine metabolites into macromolecules. Azacitidine inhibits the L1210 cells growth with IC50 and of 0.019 μg/mL. [3]
In vivo

Azacitidine inhibits polynucleotide synthesis in leukemic BDF1 mice. [3] Azacitidine (3 mg/kg, i.p.) increases the mean survival time in leukemic BDF1 mice inoculated with Ll210 ascites tumor cells. Azacitidine markedly suppresses all enzymes activity in the polyamine-biosynthetic pathway, including ornithine decarboxylase activity. putrescine-dependent S-adenosyl-L-methionine decarboxylase activity, and spermidine-dependent S-adenosyl-L-methionine decarboxylase activity. Azacitidine also inhibits the accumulations of polyamines in leukemic mice. [4]

Protocol (from reference)

Cell Assay:

[3]
  • Cell lines

    Leukemia L1210 cell

  • Concentrations

    0.15 μg/mL

  • Incubation Time

    3 days

  • 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.
Animal Study:

[4]
  • Animal Models

    BDF1 mice bearing lymphoid leukemia L1210

  • Dosages

    3 mg/kg

  • Administration

    Daily i.p. injection

Customer Product Validation

, , Cell, 2018, 172(1-2):90-105

Data from [Data independently produced by , , Epigenetics, 2015, 10(5): 431-45]

Data from [Data independently produced by , , Leuk Res, 2017, 58:91-97]

Data from [Data independently produced by , , Leuk Res, 2018, 58:91-97]

Selleck's Azacitidine (5-Azacytidine) has been cited by 115 publications

S-nitrosothiol homeostasis maintained by ADH5 facilitates STING-dependent host defense against pathogens [ Nat Commun, 2024, 15(1):1750] PubMed: 38409248
Genomic and transcriptomic profiling of peripheral T cell lymphoma reveals distinct molecular and microenvironment subtypes [ Cell Rep Med, 2024, 5(2):101416] PubMed: 38350451
Panobinostat sensitizes AraC-resistant AML cells to the combination of azacitidine and venetoclax [ Biochem Pharmacol, 2024, S0006-2952(24)00048-0] PubMed: 38373594
Nuclear translocation of cleaved PCDH9 impairs gastric cancer metastasis by downregulating CDH2 expression [ iScience, 2024, 27(2):109011] PubMed: 38357662
5-AZA Upregulates SOCS3 and PTPN6/SHP1, Inhibiting STAT3 and Potentiating the Effects of AG490 against Primary Effusion Lymphoma Cells [ Curr Issues Mol Biol, 2024, 46(3):2468-2479] PubMed: 38534772
DNA hypomethylation silences anti-tumor immune genes in early prostate cancer and CTCs [ Cell, 2023, 186(13):2765-2782.e28] PubMed: 37327786
3D genome mapping identifies subgroup-specific chromosome conformations and tumor-dependency genes in ependymoma [ Nat Commun, 2023, 14(1):2300] PubMed: 37085539
Uridine-cytidine kinase 2 potentiates the mutagenic influence of the antiviral β-d-N4-hydroxycytidine [ Nucleic Acids Res, 2023, 10.1093/nar/gkad1002] PubMed: 37953355
Aspartyl-tRNA synthetase 2 orchestrates iron-sulfur metabolism in hematopoietic stem cells via fine-tuning alternative RNA splicing [ Cell Rep, 2023, 42(10):113264] PubMed: 37838946
Sensitivity to targeted UBA1 inhibition in a myeloid cell line model of VEXAS syndrome [ Blood Adv, 2023, 7(24):7445-7456] PubMed: 38091008

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.