1. Epigenetics
  2. DNA Methyltransferase
  3. Decitabine

Decitabine (Synonyms: NSC 127716; 5-Aza-2'-deoxycytidine)

Cat. No.: HY-A0004 Purity: 99.99%
Handling Instructions

Decitabine (NSC 127716) is a DNA methyltransferase inhibitor commonly used to treat myelodysplastic syndromes (MDS) and acute myeloid leukemia (AML).

For research use only. We do not sell to patients.

Decitabine Chemical Structure

Decitabine Chemical Structure

CAS No. : 2353-33-5

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10 mM * 1 mL in DMSO USD 66 In-stock
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50 mg USD 108 In-stock
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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).

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].

Clinical Trial
Storage

4°C, protect from light

Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (219.10 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.3819 mL 21.9096 mL 43.8193 mL
5 mM 0.8764 mL 4.3819 mL 8.7639 mL
10 mM 0.4382 mL 2.1910 mL 4.3819 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (10.95 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (10.95 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (10.95 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[3]

The pyrophosphohydrolase activity of DCTPP1 is determined using a continuous spectrophotometric assay. In a standard reaction (1 mL final volum), 10-250 μM of the nucleotide substrate is incubated in reaction buffer (20 mM MgCl2, 100 mM KCl, 0.75 mg/mL BSA and 4 mM DTT) with concentrations ranging from 0.1-1 μM of DCTTP1. All reactions are carried out at 25°C.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

228.21

Formula

C₈H₁₂N₄O₄

CAS No.

2353-33-5

SMILES
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.99%

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Decitabine

Cat. No.: HY-A0004