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> Decitabine [2353-33-5]

Decitabine [2353-33-5]

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Referencia HY-A0004-1mL

embalaje : 10mM/1mL

Marca : MedChemExpress

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Descripciòn

Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and 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[5]

DNMT1

 

DNMT3A

 

DNMT3B

 

Cellular Effect
Cell Line Type Value Description References
LoVo IC50
21.9 μM
Decitabine
Compound was tested for its inhibitory activity against LoVo cells.
Compound was tested for its inhibitory activity against LoVo cells.
[PMID: 24874286]
SW111 IC50
24.2 μM
Decitabine
Compound was tested for its inhibitory activity against SW111 cells.
Compound was tested for its inhibitory activity against SW111 cells.
[PMID: 24874286]
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].

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

Decitabine Related Antibodies

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].

MedChemExpress (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.
Ensayo clínico
Peso molecular

228.21

Fòrmula

C8H12N4O4
No. CAS
Appearance

Solid

Color

White to off-white

SMILES

O[C@H]1C[C@H](N2C(N=C(N)N=C2)=O)O[C@@H]1CO
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, protect from light

*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

Solvente y solubilidad
In Vitro: 

DMSO : ≥ 50 mg/mL (219.10 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

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

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Pureza y Documentación
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