Art. -Nr.: HY-11003

GW843682X

(Synonyms: GW843682)

7 Cited Publications

Kundenbewertung

Based on 7 publication(s) in Google Scholar

GW843682X is a selective, ATP-competitive inhibitor of PLK1 and PLK3, with IC₅₀s of 2.2 nM and 9.1 nM, respectively, and is also >100-fold selective against ～30 other kinases.

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Reinheit: 99.89%
CAS. Nr.: 660868-91-7
Formel: C₂₂H₁₈F₃N₃O₄S
Molecular Weight:477.46

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GW843682X Chemical Structure

CAS. Nr.: 660868-91-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (7)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

GW843682X is a selective, ATP-competitive inhibitor of PLK1 and PLK3, with IC₅₀s of 2.2 nM and 9.1 nM, respectively, and is also >100-fold selective against ～30 other kinases.

IC₅₀ & Target^[1]

PLK1

2.2 nM (IC₅₀)

PLK3

9.1 nM (IC₅₀)

PDGFR1β

160 nM (IC₅₀)

VEGFR2

360 nM (IC₅₀)

Aurora A

4800 nM (IC₅₀)

CDK2/cyclin A

7600 nM (IC₅₀)

Alle Polo-like Kinase (PLK) Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.41 μM Compound: Chemical probe: Compound 1	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth Antiproliferative activity against human A549 cells assessed as inhibition of cell growth	[PMID: 17267659]
A549	IC₅₀	411 nM Compound: 2	Antiproliferative activity against human A549 cells after 3 days by methylene blue stain technique Antiproliferative activity against human A549 cells after 3 days by methylene blue stain technique	[PMID: 19097784]
BT-474	IC₅₀	0.57 μM Compound: Chemical probe: Compound 1	Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth	[PMID: 17267659]
HCT-116	IC₅₀	0.7 μM Compound: Chemical probe: Compound 1	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth	[PMID: 17267659]
HCT-116	IC₅₀	699 nM Compound: 2	Antiproliferative activity against human HCT116 cells after 3 days by methylene blue stain technique Antiproliferative activity against human HCT116 cells after 3 days by methylene blue stain technique	[PMID: 19097784]
HeLa	IC₅₀	0.11 μM Compound: Chemical probe: Compound 1	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth	[PMID: 17267659]
HN5	IC₅₀	0.68 μM Compound: Chemical probe: Compound 1	Antiproliferative activity against human HN5 cells assessed as inhibition of cell growth Antiproliferative activity against human HN5 cells assessed as inhibition of cell growth	[PMID: 17267659]
HN5	IC₅₀	678 nM Compound: 2	Antiproliferative activity against human HN5 cells after 3 days by methylene blue stain technique Antiproliferative activity against human HN5 cells after 3 days by methylene blue stain technique	[PMID: 19097784]
MCF7	IC₅₀	0.56 μM Compound: Chemical probe: Compound 1	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth	[PMID: 17267659]
MCF7	IC₅₀	558 nM Compound: 2	Antiproliferative activity against human MCF7 cells after 3 days by methylene blue stain technique Antiproliferative activity against human MCF7 cells after 3 days by methylene blue stain technique	[PMID: 19097784]
MES-SA	IC₅₀	0.21 μM Compound: Chemical probe: Compound 1	Antiproliferative activity against DX5 resistant human MES-SA cells assessed as inhibition of cell growth Antiproliferative activity against DX5 resistant human MES-SA cells assessed as inhibition of cell growth	[PMID: 17267659]
MES-SA	IC₅₀	0.21 μM Compound: Chemical probe: Compound 1	Antiproliferative activity against human MES-SA cells assessed as inhibition of cell growth Antiproliferative activity against human MES-SA cells assessed as inhibition of cell growth	[PMID: 17267659]
NCI-H460	IC₅₀	0.38 μM Compound: Chemical probe: Compound 1	Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth	[PMID: 17267659]
NCI-H460	IC₅₀	380 nM Compound: 2	Antiproliferative activity against human H460 cells after 3 days by methylene blue stain technique Antiproliferative activity against human H460 cells after 3 days by methylene blue stain technique	[PMID: 19097784]
NCI-N87	IC₅₀	0.6 μM Compound: Chemical probe: Compound 1	Antiproliferative activity against human NCI-N87 cells assessed as inhibition of cell growth Antiproliferative activity against human NCI-N87 cells assessed as inhibition of cell growth	[PMID: 17267659]
NCI-N87	IC₅₀	601 nM Compound: 2	Antiproliferative activity against human NCI-N87 cells after 3 days by methylene blue stain technique Antiproliferative activity against human NCI-N87 cells after 3 days by methylene blue stain technique	[PMID: 19097784]
NHDF	IC₅₀	6.14 μM Compound: Chemical probe: Compound 1	Cytotoxicity against human HDF cells assessed as inhibition of cell growth Cytotoxicity against human HDF cells assessed as inhibition of cell growth	[PMID: 17267659]
PC-3	IC₅₀	6.82 μM Compound: Chemical probe: Compound 1	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth	[PMID: 17267659]
PC-3	IC₅₀	6820 nM Compound: 2	Antiproliferative activity against human PC3 cells after 3 days by methylene blue stain technique Antiproliferative activity against human PC3 cells after 3 days by methylene blue stain technique	[PMID: 19097784]
RKO	IC₅₀	0.4 μM Compound: Chemical probe: Compound 1	Antiproliferative activity against human RKO cells assessed as inhibition of cell growth Antiproliferative activity against human RKO cells assessed as inhibition of cell growth	[PMID: 17267659]
RKO	IC₅₀	398 nM Compound: 2	Antiproliferative activity against human RKO cells after 3 days by methylene blue stain technique Antiproliferative activity against human RKO cells after 3 days by methylene blue stain technique	[PMID: 19097784]

In Vitro

GW843682X (compound 1) is effective on 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, with an IC₅₀ of 0.14 μM. GW843682X (3 μM) causes a strong G2-M arres 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^[1]. GW843682X inhibits proliferation of U937 cells with an EC₅₀ of 120 nM. GW843682X (500 nM) in combination with 5 μM VP-16 suppresses 50% of entry into mitosis in U937 cells^[2]. GW843682X (0.06-1 μM) has inhibitory activities against proliferation of acute leukemia cells, and potentiates the anti-proliferative activity of vincristine. Moreover, 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^[3].

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

Chemical Information

CAS. Nr. 660868-91-7
Appearance Solid
Molecular Weight 477.46
Formel C₂₂H₁₈F₃N₃O₄S
Color Light yellow to yellow
SMILES

O=C(C1=C(OCC2=CC=CC=C2C(F)(F)F)C=C(N3C4=CC(OC)=C(OC)C=C4N=C3)S1)N
Synonyms

GW843682
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (7)

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Journal Impact Factor

Signal Transduct Target Ther

Large-scale and high-resolution mass spectrometry-based proteomics defines molecular subtypes of nasopharyngeal carcinoma for therapeutic targeting. [Abstract]

2026 Jun 23;11(1):244. PMID: 42331772
Sci Adv

FeaSion decodes the regulatory landscape and functional diversity of RNA polymerase II CTD phosphorylation. [Abstract]

2025 Nov 28;11(48):eadz2345. PMID: 41313762
Cell Rep

miR-24 controls the regenerative competence of hair follicle progenitors by targeting Plk3. [Abstract]

2021 Jun 8;35(10):109225. PMID: 34107258
Sci Rep

Identification of Polo-like kinases as potential novel drug targets for influenza A virus. [Abstract]

2017 Aug 17;7(1):8629. PMID: 28819179
Mol Oncol

Repositioning VU-0365114 as a novel microtubule-destabilizing agent for treating cancer and overcoming drug resistance. [Abstract]

2024 Feb;18(2):386-414. PMID: 37842807
Adv Ther (Weinh)

10 September 2022.
Technical University of Dresden

2025.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 33.33 mg/mL (69.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0944 mL

10.4721 mL

20.9442 mL

5 mM

0.4189 mL

2.0944 mL

4.1888 mL

10 mM

0.2094 mL

1.0472 mL

2.0944 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 (5.24 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

PLK1 and PLK3 proteins are prepared from baculovirus-infected Trichoplusia ni cells. Enzyme activity for PLK1 and PLK3 is determined as follows. All measurements are obtained under conditions where signal production increased linearly with time and enzyme. Test compounds are added to white 384-well assay plates (0.1 μL for 10 μL and some 20 μL assays, 1 μL for some 20 μL assays) at variable known concentrations in 100% DMSO. DMSO (1-5% final) and EDTA (65 mM) are used as controls. Reaction Mix containes the following components at 22°C: 25 mM HEPES (pH 7.2); 15 mM MgCl₂; 1 μM ATP; 0.05 μCi/well [γ-³³P]ATP (10 Ci/mmol); 1 μM substrate peptide (Biotin-Ahx-SFNDTLDFD); 0.15 mg/mL bovine serum albumin; 1 mM DTT; and 2 nM PLK1 kinase domain or 5 nM full-length PLK3. Reaction Mix (10 or 20 μL) is quickly added to each well immediately following addition of enzyme via automated liquid handlers and incubated for 1 to 1.5 h at 22°C. The 20 μL enzymatic reactions are stopped with 50 μL of stop mix [50 mM EDTA, 4.0 mg/mL streptavidin SPA beads in Dulbecco's PBS (without Mg²⁺ and Ca²⁺), 50 μM ATP] per well. The 10 μL reactions are stopped with 10 μL of stop mix [50 mM EDTA, 3.0 mg/mL streptavidin-coupled SPA Imaging Beadsin Dulbecco's PBS (without Mg²⁺ and Ca²⁺), 50 μM ATP] per well. Plates are sealed, spun at 500 × g for 1 min or settled overnight, and counted in Packard TopCount for 30 s/well or imaged with a Viewlux imager. Signal above background (EDTA controls) is converted to percent inhibition relative to that obtained in control (DMSO-only) wells^[1].

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

Cell Assay^[1]

Assays are carried out and data analyzed. In these assays, H460 cells are plated at a density of 2,000 per well, HDF cells are plated at 5,000 per well, and the drug-resistant cell line MES-SA/DX5 and its sensitive parent line MES-SA are plated at 7,000 and 6,000 per well, respectively, in a 96-well plate. These densities allowed vehicle controls to grow logarithmically during the course of the 3-day assay. All cells are exposed to 3-fold dilutions of the compound (30-0.00152 μM) in low-glucose DMEM containing 5% FBS, 50 μg/mL gentamicin, and 0.3% (v/v) DMSO (HDF cells); RPMI 1640 containing 5% FBS, 50 μg/mL gentamicin, and 0.3% (v/v) DMSO (H460); or McCoy's 5A containing 5% FBS, 50 μg/mL gentamicin, and 0.3% (v/v) DMSO (MES-SA and MES-SA/DX5)^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Lansing TJ, et al. In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1. Mol Cancer Ther. 2007 Feb;6(2):450-9. Epub 2007 Jan 31. [Content Brief]

[2]. Didier C, et al. Evaluation of Polo-like Kinase 1 inhibition on the G2/M checkpoint in Acute Myelocytic Leukaemia. Eur J Pharmacol. 2008 Sep 4;591(1-3):102-5. [Content Brief]

[3]. Ikezoe T, et al. A novel treatment strategy targeting polo-like kinase 1 in hematological malignancies. Leukemia. 2009 Sep;23(9):1564-76. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0944 mL	10.4721 mL	20.9442 mL	52.3604 mL
	5 mM	0.4189 mL	2.0944 mL	4.1888 mL	10.4721 mL
	10 mM	0.2094 mL	1.0472 mL	2.0944 mL	5.2360 mL
	15 mM	0.1396 mL	0.6981 mL	1.3963 mL	3.4907 mL
	20 mM	0.1047 mL	0.5236 mL	1.0472 mL	2.6180 mL
	25 mM	0.0838 mL	0.4189 mL	0.8378 mL	2.0944 mL
	30 mM	0.0698 mL	0.3491 mL	0.6981 mL	1.7453 mL
	40 mM	0.0524 mL	0.2618 mL	0.5236 mL	1.3090 mL
	50 mM	0.0419 mL	0.2094 mL	0.4189 mL	1.0472 mL
	60 mM	0.0349 mL	0.1745 mL	0.3491 mL	0.8727 mL

Keywords

GW843682X

7 Cited Publications

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GW843682X

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) GW843682X

Alle Polo-like Kinase (PLK) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GW843682X

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) GW843682X

Alle Polo-like Kinase (PLK) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GW843682X Related Classifications

HY-11003 Related Classifications