[CAS NO. 2353-33-5]  Decitabine

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PRODUCTS SPECIFICATIONS [2353-33-5]

Catalog
HY-A0004
Brand
MCE
CAS
2353-33-5

DESCRIPTION [2353-33-5]

Overview

MDLMFCD00043011
Molecular Weight228.21
Molecular FormulaC8H12N4O4
SMILESO[C@H]1C[C@H](N2C(N=C(N)N=C2)=O)O[C@@H]1CO

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

62 Publications Citing Use of MCE


Summary

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

NCT Number Sponsor Condition Start Date Phase
NCT04283526 Novartis Pharmaceuticals|Novartis
Primary Myelofibrosis|Myelofibrosis|PMF|Post-Essential Thrombocythemia Myelofibrosis|Post-Polycythemia Vera Myelofibrosis
November 30, 2020 Phase 1
NCT01690507 Chinese PLA General Hospital|Navy General Hospital, Beijing
MDS|AML
November 2012 Phase 1|Phase 2
NCT03233724 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
Carcinoma, Non-Small-Cell Lung|Lung Cancer|Non-Small Cell Lung Cancer|Carcinoma, Esophageal|Malignant Pleural Mesotheliomas
April 11, 2018 Phase 1|Phase 2

Appearance

Solid


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 )

H 2 O : 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: PBS

    Solubility: 10 mg/mL (43.82 mM); Clear solution; Need ultrasonic

  • 2.

    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

  • 3.

    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

  • 4.

    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 available by MCE.


Synonyms

1,3,5-Triazin-2(1H)-one, 4-amino-1-(2-deoxy-β-D-erythro-pentofuranosyl)-
s-Triazin-2(1H)-one, 4-amino-1-(2-deoxy-β-D-erythro-pentofuranosyl)-
4-Amino-1-(2-deoxy-β-D-erythro-pentofuranosyl)-1,3,5-triazin-2(1H)-one
5-Aza-2′-deoxycytidine
5-Azadeoxycytidine
2-Desoxy-5-azacytidine
2′-Deoxy-5-azacytidine
Decitabine
NSC 127716
DAC
Dacogen
β-Decitabine
5-Aza-2-deoxycytidine
4-Amino-1-(2-deoxy-β-D-ribofuranosyl)-1,3,5-triazin-2(1H)-one
A 2232
NSC127716