1. Epigenetics
    Cell Cycle/DNA Damage
    Apoptosis
  2. DNA Methyltransferase
    Nucleoside Antimetabolite/Analog
    Apoptosis
  3. Decitabine

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

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

Decitabine (NSC 127716) is a deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity. DNA Methyltransferase Inhibitor.

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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Description

Decitabine (NSC 127716) is a deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity[1][2]. DNA Methyltransferase Inhibitor.

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[3].
Decitabine up-regulates DCTPP1 and dUTPase expression in HeLa cells[4].

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[5].
Decitabine (1.0 mg/kg; i.p.; once daily for 5 consecutive days) leads to regression of EL4 tumors established in C57BL/6 Mice[7].

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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Keywords:

DecitabineNSC 1277165-Aza-2'-deoxycytidineNSC127716NSC-127716DNA MethyltransferaseNucleoside Antimetabolite/AnalogApoptosisDNMTsDNA MTasesInhibitorinhibitorinhibit

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Decitabine
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