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

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

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

Décitabine (NSC 127716) est un antimétabolite analogue de désoxycytidine et un ADN méthyltransférase. Décitabine incorporée dans l'ADN à la place de la cytosine peut piéger par covalence la ADN méthyltransférase dans l'ADN, provoquant une inhibition irréversible de l'enzyme. Décitabine induit un arrêt cellulaire G2/M et l'apoptose cellulaire. Décitabine a une activité puissante anticancéreuse.

Decitabin (5-Aza-2'-Desoxycytidin) ist ein deoxycytidine analogue antimetabolite und DNA methyltransferase-Inhibitor. Decitabin wird anstelle von Cytosin in die DNA eingebaut und kann die DNA methyltransferase kovalent an die DNA binden, was zu einer irreversiblen Hemmung des Enzyms führt. Decitabin induziert den G2/M-Anhalt der Zelle und die apoptosis. Decitabin hat eine starke krebsbekämpfende Wirkung.

Decitabine (NSC 127716) is an orally active 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.

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Decitabine Chemical Structure

Decitabine Chemical Structure

CAS No. : 2353-33-5

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Description

Decitabine (NSC 127716) is an orally active 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].

IC50 & 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].
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].

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

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].

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

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)

H2O : 20 mg/mL (87.64 mM; Need ultrasonic)

*"≥" 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:

Decitabine5-Aza-2'-deoxycytidine 5-AZA-CdR NSC 127716NSC127716NSC 127716NSC-127716DNA MethyltransferaseApoptosisNucleoside Antimetabolite/AnalogDNMTsDNA MTasesInhibitorinhibitorinhibit

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