Catalog No.S1200 Synonyms: Deoxycytidine
Molecular Weight(MW): 228.21
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).
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(A) and (B) SW1116 and LOVO cells were plated, treated for 48 h with decitabine (DAC) and gefitinib (GEF) either alone or in combination, and the expression levels of AKT, mTOR, S6K, and phosphorylation were determined by Western blot analysis as described under Methods. Expression of β-actin served as a loading control. The data are representative of three independent experiments.
PLoS One 2014 9(5), e97719. Decitabine purchased from Selleck.
(A) and (B) SW1116 and LOVO cells were cultured in control conditions (DMSO) or in the presence of the indicated concentrations of decitabine (DAC) and gefitinib (GEF), alone or in combination, for 48 h. And then cells were stained with Annexin V-FITC and propidium iodide (PI) and analyzed by flow cytometry. This experiment was done in triplicate and representative diagrams of Annexin V-FITC assays are shown.
PLoS One 2014 9(5), e97719. Decitabine purchased from Selleck.
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|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 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.  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. 
|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. |
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.
|In vitro||DMSO||45 mg/mL (197.18 mM)|
|Water||10 mg/mL (43.81 mM)|
|In vivo||30% propylene glycol, 5% Tween 80, 65% D5W||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02839694||Recruiting||Neoplasm Metastasis|Sarcoma|Neoplasms, Germ Cell and Embryonal|Melanoma||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||July 7, 2016||Phase 1|
|NCT01479348||Enrolling by invitation||Head and Neck Neoplasms|Lung Neoplasms|Urinary Bladder Neoplasms|Breast Neoplasms||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||October 28, 2011||Early Phase 1|
|NCT03041688||Not yet recruiting||Recurrent Adult Acute Myeloid Leukemia|Secondary Acute Myeloid Leukemia|TP53 wt Allele|Untreated Adult Acute Myeloid Leukemia||National Cancer Institute (NCI)||October 2017||Phase 1|
|NCT03009240||Not yet recruiting||Recurrent Adult Acute Myeloid Leukemia|Recurrent Childhood Acute Myeloid Leukemia|Secondary Acute Myeloid Leukemia|Therapy-Related Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia||City of Hope Medical Center|National Cancer Institute (NCI)||June 2017||Phase 1|
|NCT02890329||Not yet recruiting||Chimerism|Hematopoietic Cell Transplantation Recipient|Myelodysplastic Syndrome With Excess Blasts-1|Myelodysplastic Syndrome With Excess Blasts-2|Previously Treated Myelodysplastic Syndrome|Recurrent Adult Acute Myeloid Leukemia|Secondary Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia||National Cancer Institute (NCI)||April 2017||Phase 1|
|NCT02847000||Not yet recruiting||Metastatic Pancreatic Adenocarcinoma||Yogen Saunthararajah|Case Comprehensive Cancer Center||March 2017||Early Phase 1|
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