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GW843682X

Name: GW843682X
Brand: TargetMol
SKU: T15454
Price: 32 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T15454Cas No. 660868-91-7

Alias GW843682

GW843682X (GW843682) is a selective and ATP-competitive inhibitor of PLK1 and PLK3 (IC50s = 2.2 nM and 9.1 nM).

GW843682X

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Purity: 99.92%

Catalog No. T15454Alias GW843682Cas No. 660868-91-7

GW843682X (GW843682) is a selective and ATP-competitive inhibitor of PLK1 and PLK3 (IC50s = 2.2 nM and 9.1 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$32	In Stock	In Stock
2 mg	$45	In Stock	In Stock
5 mg	$74	In Stock	In Stock
10 mg	$129	In Stock	In Stock
25 mg	$259	In Stock	In Stock
50 mg	$396	-	In Stock
1 mL x 10 mM (in DMSO)	$81	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.92%

Appearance:Solid

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	GW843682X (GW843682) is a selective and ATP-competitive inhibitor of PLK1 and PLK3 (IC50s = 2.2 nM and 9.1 nM).
Targets&IC50	CDK2-CyclinA:7600 nM, PDGFR1β:160 nM, VEGFR2:360 nM, PLK3:9.1 nM, Aurora A:4800 nM, PLK1:2.2 nM
In vitro	GW843682X (500 nM) in combination with 5 µM VP-16 suppresses 50% of entry into mitosis in U937 cells. GW843682X inhibits the proliferation of U937 cells with an EC50 of 120 nM[1]. GW843682X (0.06-1 μM) has inhibitory activities against the proliferation of acute leukemia cells and potentiates the anti-proliferative activity of vincristine. GW843682X (0.1-1 μM) induces apoptosis of leukemia cells in a dose- and time-dependent manner. GW843682X (0.5-1 μM) dephosphorylates Bcl-xl in leukemia cells[2]. GW843682X is effective in inhibition of growth of tumor cells, with IC50s of 0.41, 0.57, 0.11, 0.38, and 0.70 μM for A549, BT474, HeLa, H460 and HCT116 cell lines. GW843682X dose-dependently inhibits PLK1 phosphorylation of Ser15-p53 (IC50 = 0.14 μM). GW843682X (3 μM) causes strong G2-M arrest in HDF cells and H460 cells after treatment for 24, 48, and 72 h. GW843682X (5 μM) leads to apoptosis in H460 cells instead of HDF cells[3].
Synonyms	GW843682

Chemical Properties

Molecular Weight	477.46
Formula	C₂₂H₁₈F₃N₃O₄S
Cas No.	660868-91-7
Smiles	COc1cc2ncn(-c3cc(OCc4ccccc4C(F)(F)F)c(s3)C(N)=O)c2cc1OC
Relative Density.	1.45 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 30 mg/mL (62.83 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 2 mg/mL (4.19 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	2.0944 mL	10.4721 mL	20.9442 mL	104.7208 mL
5 mM	0.4189 mL	2.0944 mL	4.1888 mL	20.9442 mL
10 mM	0.2094 mL	1.0472 mL	2.0944 mL	10.4721 mL
20 mM	0.1047 mL	0.5236 mL	1.0472 mL	5.2360 mL
50 mM	0.0419 mL	0.2094 mL	0.4189 mL	2.0944 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:

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