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5-Aza-2'-deoxycytidine
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Product Name 5-Aza-2'-deoxycytidine
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Catalog No.: CN02011
CAS No.: 2353-33-5
Molecular Formula: C8H12N4O4
Molecular Weight: 228.21 g/mol
Purity: >=98%
Type of Compound: Alkaloids
Physical Desc.: Powder
Source:
Solvent: DMSO, Pyridine, Methanol, Ethanol, etc.
SMILES: OC[C@H]1O[C@H](C[C@@H]1O)n1cnc(nc1=O)N
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Description Decitabine (NSC 127716) is a DNA methyltransferase inhibitor commonly used to treat myelodysplastic syndromes (MDS) and acute myeloid leukemia (AML).
Target DNMT1 DNMT3A DNMT3B
In Vitro Decitabine treatment significantly inhibits cell growth of SNU719, NCC24 and KATOIII 96 hours after exposure to decitabine. Decitabine induces G2/M arrest and apoptosis in EBVaGC, inhibits invasion ability, and up-regulates E-cadherin expression for EBVaGC[1]. Tri-acetylation on the H4 N-terminal tail (H4K8acK12acK16ac) is reduced after DAC treatment in MDS-L sensitive cells[2]. Decitabine up-regulates DCTPP1 and dUTPase expression in HeLa cells[3].
In Vivo Decitabine (1.0 mg/kg, p.o.) in combination with tetrahydrouridine (THU) causes severe toxicity occurs in females, and results in an increased sensitivity to decitabine toxicity correlating with decitabine plasma levels[4].
Cell Assay Cell viability is analyzed by cell count and MTS assay. SNU719, NCC24 and KATOIII are seeded at a density of 5×104 cells/mL and cultured with only RPMI-1640 supplemented with FBS for 24 hours. After 24 hours of incubation, cells are treated in the presence or absence of Decitabine (DAC) for 120 hours. Cells for cell counts are trypsinized and counted at 0, 24, 48, 72, 96 and 120 hours after DAC treatment. Viable cells are determined by trypan blue exclusion. For MTS assay, cells (SNU719 and NCC24: 1x104/well, KATOIII: 1x103/well) are eeded onto 96-well dishes. After seeding, MTS is added into the well at the indicated period. After incubation for 1 hour, the absorbance is measured at 490 nm.
Animal Admin Mice are assigned to four dose groups and a vehicle control group. Animals are gavaged with Decitabine (DAC) or its vehicle 1 hour ± 5 minutes after administration of tetrahydrouridine (THU) or its vehicle at a dose volume of 10 mL/kg. The DAC doses are selected based on the range finding study in which the mice tolerated six oral doses (2x/week) of 0.1, 0.2 and 0.4 mg/kg DAC in combination with a fixed dose of 167 mg/kg THU. A fixed THU dose (500 mg/m2) and the optimal timing between THU and DAC administration (60 min) are selected. Conversion of milligrams per body surface area dose in mice into milligrams per kilogram body weight dose estimation is based on Michaelis constant (Km) values for mice. In brief, the mouse dose in milligrams per body surface area (500 mg/m2) is divided by the Km of 3 to convert the dose to milligrams per kilogram body weight (167 mg/kg). The working body weight range of mice in the guideline is 11-34 gram; the body weight range of mice used in this study is 24-38 gram.
Density1.9±0.1 g/cm3
Boiling Point485.8±55.0 °C at 760 mmHg
Flash Point247.6±31.5 °C
Exact Mass228.085861
PSA123.49000
LogP-1.93
Vapour Pressure0.0±2.8 mmHg at 25°C