Decitabine

Catalog No.S1200
5 5 3 Product Citations

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

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Decitabine Chemical Structure

Decitabine Chemical Structure
Molecular Weight: 228.21

Validation & Quality Control

Customer Reviews(3)

Quality Control & MSDS

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Product Information

  • Compare DNA Methyltransferase Inhibitors
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  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

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 (KG1a cells) [1] DNA methyltransferase (HL-60 cells) [1]
IC50 1 ng/mL 100 ng/mL
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]
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.
Solubility 30% propylene glycol, 5% Tween 80, 65% D5W, 30 mg/mL
* 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Shaker S, et al. Leuk Res, 2003, 27(5), 437-444.

[2] Hassler MR, et al. Biochimie, 2012, doi.org/10.1016/j.biochi.2012.05.029.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-11-22)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02141477 Not yet recruiting Leukemia M.D. Anderson Cancer Center|Teva Pharmaceuticals USA December 2014 Phase 2
NCT02257138 Not yet recruiting Leukemia|Myeloproliferative Diseases M.D. Anderson Cancer Center|Incyte Corporation December 2014 Phase 1|Phase 2
NCT02172872 Not yet recruiting Acute Myeloid Leukemia (AML)|Decitabine European Organisation for Research and Treatment of Cance  ...more European Organisation for Research and Treatment of Cancer - EORTC|Janssen Pharmaceuticals|Gruppo Italiano Malattie EMatologiche dellAdulto December 2014 Phase 3
NCT02269280 Recruiting Leukemia M.D. Anderson Cancer Center|MDS Consortium October 2014 Phase 2
NCT02252107 Recruiting Acute Myeloid Leukemia (AML) Radboud University October 2014 Phase 2

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Chemical Information

Download Decitabine SDF
Molecular Weight (MW) 228.21
Formula

C8H12N4O4

CAS No. 2353-33-5
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms Deoxycytidine
Solubility (25°C) * In vitro DMSO 45 mg/mL (197.18 mM)
Water 10 mg/mL (43.81 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W 30 mg/mL
* <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.
Chemical Name 4-amino-1-((2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)-1,3,5-triazin-2(1H)-one

Research Area

Customer Reviews (3)


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Rating
Source PLoS One 2014 9(5), e97719. Decitabine purchased from Selleck
Method Western blot
Cell Lines SW1116, LOVO cells
Concentrations 10 uM
Incubation Time 48 h
Results Decitabine (10 uM) could not lead to significant alterations in AKT, or mTOR activity, as assessed by Western blot for phosphorylation of AKT, mTOR and S6K. Additionally, it observed minimal reductions of phosphorylation of AKT, mTOR and S6K with 5 uM gefitinib in SW1116 and 4 礛 in LOVO cells. However, the combination of decitabine and gefitinib completely abrogated AKT and mTOR activities in SW1116 and LOVO cells.

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Rating
Source PLoS One 2014 9(5), e97719. Decitabine purchased from Selleck
Method Annexin V-FITC/PI analysis
Cell Lines SW1116, LOVO cells
Concentrations 10 uM
Incubation Time 48 h
Results SW1116 and LOVO cells were treated with the two compounds, alone or in combination, for 48 h and then cell apoptosis was determined by Annexin V-FITC and propidium iodide (PI) staining and flow cytometry analysis. Treatment with gefitinib (2 uM) or decitabine (10 uM) alone had weak effects on apoptosis in SW1116 cells. However, there was a significantly higher apoptosis rate found upon treatment with the combination of gefitinib and decitabine.

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Rating
Source Leuk Res 2014 38(3), 402-10. Decitabine purchased from Selleck
Method Bisulfite sequencing analysis
Cell Lines NB4 cells
Concentrations 10 uM
Incubation Time 24 h
Results Mature miR-125a expression increased with increasing amounts of decitabine treatment after 24 hours.

Product Citations (3)

Tech Support & FAQs

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