Biological Activity
Selective inhibitor of polo-like kinase 1 (PLK1) and polo-like kinase 3 (PLK3) (IC50 values are 2.2 and 9.1 nM respectively). Displays > 100-fold selectivity over ~30 other kinases tested including cdk1 and cdk2. Inhibits proliferation of most tumor cells in vitro and is selective over normal diploid fibroblasts.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Compound Libraries
GW 843682X is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 477.46 |
| Formula | C22H18F3N3O4S |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 660868-91-7 |
| PubChem ID | 9826308 |
| InChI Key | JSKUWFIZUALZLX-UHFFFAOYSA-N |
| Smiles | O=C(N)C(S3)=C(OCC4=CC=CC=C4C(F)(F)F)C=C3N2C1=CC(OC)=C(OC)C=C1N=C2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 35.81 | 75 | |
| ethanol | 2.39 | 5 |
Preparing Stock Solutions
The following data is based on the product molecular weight 477.46. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.09 mL | 10.47 mL | 20.94 mL |
| 5 mM | 0.42 mL | 2.09 mL | 4.19 mL |
| 10 mM | 0.21 mL | 1.05 mL | 2.09 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Lansing et al (2007) In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1. Mol.Cancer Ther. 6 450 PMID: 17267659
Keywords: GW 843682X, supplier, Selective, inhibitors, inhibits, PLK1, PLK3, Mitosis, Polo-like, Kinases, GW843682X, GlaxoSmithKline, GSK, Polo-like, Kinase, Mitosis, Polo-like, Kinase, Tocris Bioscience
