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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Description

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

IC50 & Target[5]

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].
Only high concentrations (10 µM) Decitabine (0.1-1 μM; 24-72 hours) results in a G2 phase arrest, which is accompanied by a reduction of cells in G1 phase[2].
Decitabine up-regulates DCTPP1 and dUTPase expression in HeLa cells[3].

Cell Cycle Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.1, 1, 10 µM
Incubation Time: 24, 48, 72 hours
Result: Only high drug concentrations (10 µM) resulted in a G2 phase arrest, which was accompanied by a reduction of cells in G1 phase.
In Vivo

Decitabine (1.0 mg/kg, p.o.) in combination with tetrahydrouridine (THU) causes severe toxicity occurs in female CD-1 mice, and results in an increased sensitivity to decitabine toxicity correlating with decitabine plasma levels[4].
Decitabine (1.0 mg/kg; i.p.; once daily for 5 consecutive days) leads to regression of EL4 tumors established in C57BL/6 Mice[6].

Animal Model: C57BL/6 mice (bearing EL4 cells)[6]
Dosage: 1.0 mg/kg
Administration: Intraperitoneal injection; once daily for 5 consecutive days
Result: Caused continuous tumor regression even after Decitabine treatment was stopped.
Clinical Trial
Molecular Weight

228.21

Formula

C₈H₁₂N₄O₄

CAS No.

2353-33-5

SMILES
Shipping

Room temperature in continental US; may vary elsewhere

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (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

Purity: 99.99%

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Decitabine
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