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GSK3685032

Name: GSK3685032
Brand: TargetMol
SKU: T9573
Price: 73 USD
Availability: InStock
Rating: 5 (10 reviews)

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Synonyms:

Catalog No. T9573 Copy Product Info

Purity: 99.49%

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GSK3685032 is a time-independent, non-covalent, selective, and reversible DNMT1 inhibitor with an IC₅₀ of 0.036 μM. GSK3685032 induces loss of DNA methylation, transcriptional activation, and inhibition of cancer cell growth, and can be used in cancer therapy research.

Cas No. 2170137-61-6

Pack Size	Price	USA Stock	Global Stock
1 mg	$73	In Stock	In Stock
2 mg	$107	In Stock	In Stock
5 mg	$179	In Stock	In Stock
10 mg	$287	In Stock	In Stock
25 mg	$539	In Stock	In Stock
50 mg	$769	In Stock	In Stock
100 mg	$1,050	In Stock	In Stock
200 mg	$1,410	-	In Stock
1 mL x 10 mM (in DMSO)	$190	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.49%

Appearance:Solid

Color:White to Yellow

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COA HNMR HPLC

Product Introduction

Bioactivity

Description	GSK3685032 is a time-independent, non-covalent, selective, and reversible DNMT1 inhibitor with an IC₅₀ of 0.036 μM. GSK3685032 induces loss of DNA methylation, transcriptional activation, and inhibition of cancer cell growth, and can be used in cancer therapy research.
Targets & IC50	DNMT1:36 nM, MM.IR cells:0.64 μM, Ki-JK cells:0.64 μM, EOL-1 cells:0.64 μM
In vitro	Methods: HCT-116 cells were treated with GSK3685032 at gradient concentrations (0.1 μM, 1 μM, 10 μM) for 72 hours, followed by DNA methylation level detection via sulfite sequencing. Results: GSK3685032 dose-dependently reduced global and promoter region DNA methylation. [1] Methods: Wild-type mESCs were treated with 2 μM and 10 μM GSK3685032 for 2, 4, 6, 8, 10, 12, and 14 days. RT-qPCR was used to detect genes known to be regulated by methylation. Results: Significant upregulation of methylation-regulated genes was observed after just 2 days of GSK3685032 treatment. [2]
In vivo	Methods: MV-4-11 AML cells were subcutaneously implanted into nude mice. After tumors became palpable, mice were randomly assigned to treatment groups. GSK3685032 was administered orally once daily at doses of 25, 50, and 100 mg/kg for 21 days. Results: GSK3685032 exhibited dose-dependent inhibition of tumor growth and induced tumor regression at the 100 mg/kg dose. [1]

Chemical Properties

Molecular Weight	420.53
Formula	C₂₂H₂₄N₆OS
Cas No.	2170137-61-6
Smiles	CCc1c(C#N)c(SC(C(N)=O)c2ccccc2)nc(N2CCC(N)CC2)c1C#N
Relative Density.	1.33 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 26.4 mg/mL (62.78 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.76 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

	1mg	5mg	10mg	50mg
1 mM	2.3780 mL	11.8898 mL	23.7795 mL	118.8976 mL
5 mM	0.4756 mL	2.3780 mL	4.7559 mL	23.7795 mL
10 mM	0.2378 mL	1.1890 mL	2.3780 mL	11.8898 mL
20 mM	0.1189 mL	0.5945 mL	1.1890 mL	5.9449 mL
50 mM	0.0476 mL	0.2378 mL	0.4756 mL	2.3780 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 µL PEG300 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 ddH₂O TargetMol | 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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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