Decitabine
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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Leuk Res 2014 38(3), 402-10. Decitabine purchased from Selleck.
Purity & Quality Control
Choose Selective DNA Methyltransferase Inhibitors
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). | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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] |
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| Cell Data |
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| 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
| Kinase Assay:[1] |
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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. |
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| Cell Research:[1] |
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| Animal Research:[2] |
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Solubility (25°C)
| In vitro | DMSO | 45 mg/mL (197.18 mM) |
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| Water | 10 mg/mL (43.81 mM) | |
| Ethanol | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): water For best results, use promptly after mixing. |
10mg/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.
Chemical Information
| Molecular Weight | 228.21 |
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| Formula | C8H12N4O4 |
| CAS No. | 2353-33-5 |
| Storage | powder |
| in solvent | |
| Synonyms | Deoxycytidine |
Bio Calculators
Molarity Calculator
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
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| NCT03709550 | Not yet recruiting | Castration Levels of Testosterone|Castration-Resistant Prostate Carcinoma|Metastatic Prostate Carcinoma in the Soft Tissue|Prostate Carcinoma Metastatic in the Bone|PSA Level Greater Than or Equal to Two|PSA Progression|Stage IV Prostate Cancer AJCC v8|Stage IVA Prostate Cancer AJCC v8|Stage IVB Prostate Cancer AJCC v8 | Roswell Park Cancer Institute|National Cancer Institute (NCI) | November 30 2018 | Phase 1|Phase 2 |
| NCT03691376 | Not yet recruiting | HLA-A*0201 Positive Cells Present|HLA-DP4 Positive Cells Present|Platinum-Resistant Ovarian Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Refractory Fallopian Tube Carcinoma|Refractory Ovarian Carcinoma|Refractory Primary Peritoneal Carcinoma | Roswell Park Cancer Institute|National Cancer Institute (NCI) | November 25 2018 | Phase 1 |
| NCT03661307 | Recruiting | Acute Myeloid Leukemia With FLT3/ITD Mutation|Blasts More Than 10 Percent of Bone Marrow Nucleated Cells|Blasts More Than 10 Percent of Peripheral Blood White Cells|Myelodysplastic Syndrome|Recurrent Acute Myeloid Leukemia|Recurrent Myelodysplastic Syndrome | M.D. Anderson Cancer Center|National Cancer Institute (NCI) | October 31 2018 | Phase 1|Phase 2 |
| NCT03679650 | Recruiting | Acute Myelogenous Leukemia | Dana-Farber Cancer Institute|National Cancer Institute (NCI) | October 11 2018 | Phase 1 |
| NCT03252457 | Not yet recruiting | Purpura Thrombocytopenic Idiopathic|Immune Thrombocytopenia | Shandong University|Second Affiliated Hospital of Medical College Shandong University|Shandong Provincial Hospital|Qingdao Central Hospital|Chinese Academy of Medical Sciences | September 1 2018 | Phase 3 |
| NCT03593915 | Recruiting | Myelodysplastic Syndromes (MDS) | Tolero Pharmaceuticals Inc. | August 29 2018 | Phase 1|Phase 2 |
Tech Support
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.
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Frequently Asked Questions
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Question 1:
Is S1200 a racemic mixture or a monomer?
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Answer:
S1200 is R form
