Decitabine

Catalog No.S1200 Batch:S120013

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Technical Data

Formula

C8H12N4O4
Molecular Weight 228.21 CAS No. 2353-33-5
Solubility (25°C)* In vitro DMSO 46 mg/mL (201.56 mM)
Water 46 mg/mL (201.56 mM)
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
water
10.0mg/ml Taking the 1 mL working solution as an example, add 10 mg of this product to 1 ml of ddH2O, mix evenly to make it clear, 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.)

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Biological Activity

Description Decitabine is a DNA methyltransferase inhibitor, incorporating into DNA and resulting in hypomethylation of DNA and intra-S-phase arrest of DNA replication. It is used to treat myelodysplastic syndrome (MDS). Decitabine induces cell cycle arrest and apoptosis in various cancer cell lines.
Targets
DNA methylation [1]
(HL-60, KG1a cells)
In vitro

Decitabine inhibits cell growth in a dose and time-dependent manner with IC50 of approximately 438 nM and 43.8 nM for 72 hours and 96 hours exposure in HL-60 and KG1a leukemic cells, respectively. [1] A recent study shows that Decitabine exhibits high anti-proliferative and pro-apoptotic activity against anaplastic large cell lymphoma (ALCL), and inhibits [3H]–thymidine uptake in KARPAS-299 cells with EC50 of 0.49 μM. [2]
In vivo

In a ALK+ KARPAS-299 murine xenograft model, Decitabine at a dose of 2.5 mg/kg causes increased apoptosis and reduced proliferation of tumor cells, and also results in demethylation of tumor suppressor p16INK4A. [2]

Protocol (from reference)

Kinase Assay:

[1]
  • DNA synthesis assay

    The rate of DNA synthesis is measured by the incorporation of radioactive thymidine into DNA. HL-60 and KG1a cells are suspended in 2 mL RPMI medium containing 10% fetal serum in 6-well (35 mm diameter) dishes and incubated with different concentrations of corresponding drugs for 48 hours (drugs are added simultaneously). At 48 hours, 0.5 μCi [3H] thymidine (6.7 Ci/mmol) is added to each well and incubated for an additional 24 hours. The cells are placed on GF/C glass fiber filters (2.4 cm diameter), washed with cold 0.9% NaCl, 5% cold trichloroacetic acid and ethanol. The filters containing the DNA are then dried, placed in EcoLite scintillation liquid (ICN) and the radioactivity measured using Beckman LS 6000IC scintillation counter. The IC50 is defined as the concentration of drug that inhibits 50% of the DNA synthesis of the leukemic cell lines from the dose–response curve.
Cell Assay:

[1]
  • Cell lines

    HL-60 and KG1a

  • Concentrations

    0-500 nM

  • Incubation Time

    96 hours

  • Method

    For the growth inhibition assay, cells in log phase are placed in 5 mL of medium. Different concentrations of Decitabine are added to the medium simultaneously. Cell counts are performed at the indicated times using a model ZM Coulter Counter. The concentration that produces 50% inhibition of growth (IC50) is determined from the growth curves of the drug treated leukemic cell lines.
Animal Study:

[2]
  • Animal Models

    KARPAS-299 human cells are inoculated subcutaneously into the right and left flanks of the mice.

  • Dosages

    ≤2.5 mg/kg

  • Administration

    Administered via i.p.

Customer Product Validation

Data from [Data independently produced by PLoS One, 2014, 9(5), e97719]

Data from [Data independently produced by PLoS One, 2014, 9(5), e97719]

Data from [Leuk Res, 2014, 38(3), 402-10]

Selleck's Decitabine has been cited by 190 publications

Genomic and transcriptomic profiling of peripheral T cell lymphoma reveals distinct molecular and microenvironment subtypes [ Cell Rep Med, 2024, 5(2):101416] PubMed: 38350451
A functional personalised oncology approach against metastatic colorectal cancer in matched patient derived organoids [ NPJ Precis Oncol, 2024, 8(1):52] PubMed: 38413740
EFNB1 levels determine distinct drug response patterns guiding precision therapy for B-cell neoplasms [ iScience, 2024, 27(1):108667] PubMed: 38155773
Targeting G9a/DNMT1 methyltransferase activity impedes IGF2-mediated survival in hepatoblastoma [ Hepatol Commun, 2024, 8(2)e0378] PubMed: 38285887
TERT promoter methylation is associated with high expression of TERT and poor prognosis in papillary thyroid cancer [ Front Oncol, 2024, 14:1325345] PubMed: 38313800
Decitabine combined with cold atmospheric plasma induces pyroptosis via the ROS/Caspase-3/GSDME signaling pathway in Ovcar5 cells [ Biochim Biophys Acta Gen Subj, 2024, 1868(6):130602] PubMed: 38513927
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
DNMT1 mediates the disturbed flow-induced endothelial to mesenchymal transition through disrupting β-alanine and carnosine homeostasis [ Theranostics, 2023, 13(13):4392-4411] PubMed: 37649604
DNMT1 mediates the disturbed flow-induced endothelial to mesenchymal transition through disrupting β-alanine and carnosine homeostasis [ Theranostics, 2023, 13(13):4392-4411] PubMed: 37649604
Targeting polycomb repressor complex 2-mediated bivalent promoter epigenetic silencing of secreted frizzled-related protein 1 inhibits cholangiocarcinoma progression [ Clin Transl Med, 2023, 13(12):e1502] PubMed: 38050190

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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.

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