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Decitabine

Decitabine is a potent inhibitor of DNA methylation with IC50 of 438 nM and 4.38 nM in HL-60 and KG1a cells, respectively.

Catalog No.S1200
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Decitabine Chemical Structure

Decitabine Chemical Structure
Molecular Weight: 228.21

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Decitabine is available in the following compound libraries:

Inhibitor Library (96-well) FDA Approved Drug Library (96-well) Chemotherapeutic Agent Library (96-well) Chemical Library (96-well) Cambridge Cancer Compound Library(96-well)

Product Information

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Product Description

Biological Activity Protocol Chemical Information Tech Support & FAQs

Biological Activity

Description Decitabine is a potent inhibitor of DNA methylation with IC50 of 438 nM and 4.38 nM in HL-60 and KG1a cells, respectively.
Targets DNA methyltransferase (HL-60) DNA methyltransferase (KG1a)
IC50 100 ng/mL 1 ng/mL [1]
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]
Clinical Trials Decitabine is currently in Phase I clinical trials in patients with Higher-risk MDS and MDS/AML Receiving Allogeneic Stem Cell Transplantation.
Features

Protocol(Only for 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.
Formulation Decitabine is dissolved in sterile PBS .
Dosages ≤2.5 mg/kg
Administration Administered via i.p.
1

References

Chemical Information

Download Decitabine SDF
Molecular Weight (MW) 228.21
Formula

C8H12N4O4
CAS No. 2353-33-5
Synonyms Dacogen
Solubility (25°C)
  • DMSO 46 mg/mL
  • Water 10 mg/mL
  • Ethanol 2 mg/mL
Storage 2 years -20°CPowder
2 weeks4°Cin DMSO
6 months-80°Cin DMSO
Chemical Name 4-amino-1-((2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)-1,3,5-triazin-2(1H)-one
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Research Area

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions
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  • SGI-110

    SGI-110 is a second generation DNA-hypomethyating agent.

  • Zebularine

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  • Panobinostat (LBH589)

    LBH589 (Panobinostat) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM and 20 nM in MOLT-4 and Reh cells, respectively.

  • Trichostatin A (TSA)

    Trichostatin A (TSA) is an HDAC inhibitor with IC50 of ~1.8 nM.

  • Entinostat (MS-275, SNDX-275)

    MS-275 is an HDAC inhibitor of HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM, respectively.

  • Belinostat (PXD101)

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  • LAQ824 (NVP-LAQ824, Dacinostat)

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