product name Decitabine
Description: Decitabine is a potent inhibitor of DNA methylation, used to treat myelodysplastic syndrome (MDS). Decitabine is a kind of deoxycytidine analog and an inducer of cellular differentiation. Decitabine has been shown substantial efficacy in reactivating epigenetically silenced tumor suppressor genes in vitro. In T24 bladder cancer cells, decitabine can increase histone H3-lysine 9 acetylation and histone H3-lysine 4 methylation at the unmethylated p14 promoter.
References: Leuk Res. 2003 May;27(5):437-44; Biochimie. 2012 Nov;94(11):2297-307.
228.21
Formula
C8H12N4O4
CAS No.
2353-33-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 45 mg/mL (197.2 mM)
Water: 10 mg/mL (43.8 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
Synonyms
Deoxycytidine
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19410622
| In Vitro |
In vitro activity: 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. Kinase 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: 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 line (HL-60 and KG1a). |
|---|---|
| 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. |
| Animal model | KARPAS-299 human cells are inoculated subcutaneously into the right and left flanks of the mice. |
| Formulation & Dosage | Dissolved in PBS; 2.5 mg/kg; i.p. injection |
| References | Leuk Res. 2003 May;27(5):437-44; Biochimie. 2012 Nov;94(11):2297-307. |
