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Guadecitabine sodium

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Catalog No. T12790Cas No. 929904-85-8
Alias SGI-110 sodium, S-110 sodium

Guadecitabine sodium is a inhibitor of second-generation DNA methyltransferases (DNMT) .

Guadecitabine sodium

Guadecitabine sodium

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Catalog No. T12790Alias SGI-110 sodium, S-110 sodiumCas No. 929904-85-8
Guadecitabine sodium is a inhibitor of second-generation DNA methyltransferases (DNMT) .
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
25 mg$1,6706-8 weeks6-8 weeks
50 mg$2,1806-8 weeks6-8 weeks
100 mg$2,8006-8 weeks6-8 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
Guadecitabine sodium is a inhibitor of second-generation DNA methyltransferases (DNMT) .
In vitro
Treatment of HCT116 colorectal carcinoma cells with Guadecitabine sodium (SGI-110 sodium) demonstrated a dose-dependent increase in p16 expression after 6 days. Additionally, there was a similar increase in p16 protein levels in both T24 and HCT116 cells when treated with Guadecitabine sodium or 5-aza-CdR for 3 days. This effect suggests Guadecitabine sodium's effectiveness in inhibiting DNA methylation and stimulating p16 expression at both mRNA and protein levels, akin to 5-aza-CdR. Further, Guadecitabine sodium inhibited DNA methylation in the 5′-region and induced the expression of the p16 gene in T24 and HCT116 cells at concentrations comparable to those of 5-aza-CdR. The induction of p16 expression by both agents was associated with demethylation at the 5′-end region of the gene in both cell lines. In terms of toxicity, Guadecitabine sodium was slightly less toxic than 5-aza-CdR at concentrations up to 1 μM, but displayed similar toxicity levels at 10 μM concentration[1].
In vivo
Guadecitabine sodium (10mg/kg) effectively reduces DNA methylation, retards tumor growth, and demonstrates a toxicity level comparable to 5-Aza-CdR. It successfully reactivates the expression of the heavily methylated p16 gene in parent EJ6 cells and reduces DNA methylation at the p16 promoter region in vivo. Notably, Guadecitabine sodium exhibits better tolerance compared to 5-Aza-CdR in vivo[2].
SynonymsSGI-110 sodium, S-110 sodium
Chemical Properties
Molecular Weight580.407
FormulaC18H24N9NaO10P
Cas No.929904-85-8
Smiles[Na].[H][C@@]1(C[C@H](O)[C@@H](COP(O)(=O)O[C@H]2C[C@@]([H])(O[C@@H]2CO)n2cnc(N)nc2=O)O1)n1cnc2c1[nH]c(N)nc2=OjcExt:v:0:0
Relative Density.1.31g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 50 mg/mL (86.15 mM), Sonication is recommended.
H2O: Soluble
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.5 mg/mL (4.31 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.7229 mL8.6146 mL17.2293 mL86.1464 mL
5 mM0.3446 mL1.7229 mL3.4459 mL17.2293 mL
10 mM0.1723 mL0.8615 mL1.7229 mL8.6146 mL
20 mM0.0861 mL0.4307 mL0.8615 mL4.3073 mL
50 mM0.0345 mL0.1723 mL0.3446 mL1.7229 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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