Biological Activity
Potent dual EGFR/ErbB2 tyrosine kinase inhibitor (IC50 values are 0.01 and 0.014 μM respectively). Selectively inhibits growth of human tumor cells overexpressing EGFR and ErbB2 (IC50 values are 0.11 μM for inhibition of HN5, N87 and BT474 tumor cell lines vs. > 30 μM for inhibition of non-tumor cell line HFF). Inhibits tumor growth in vivo by ~ 80% in a murine xenograft model following oral administration.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline.
Compound Libraries
GW 583340 dihydrochloride 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 | 671.03 |
| Formula | C28H25ClFN5O3S2.2HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 1173023-85-2 |
| PubChem ID | 16219404 |
| InChI Key | WIMITXDBYLKRKB-UHFFFAOYSA-N |
| Smiles | Cl.Cl.CS(=O)(=O)CCNCC1=NC(=CS1)C1=CC=C2N=CN=C(NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)C2=C1 |
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 | 67.1 | 100mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 671.03. 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 | 1.49 mL | 7.45 mL | 14.9 mL |
| 5 mM | 0.3 mL | 1.49 mL | 2.98 mL |
| 10 mM | 0.15 mL | 0.75 mL | 1.49 mL |
| 50 mM | 0.03 mL | 0.15 mL | 0.3 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Gaul et al (2003) Discovery and biological evaluation of potent dual ErbB-2/EGFR tyrosine kinase inhibitors: 6-thiazolylquinazolines. Bioorg.Med.Chem.Lett. 13 637 PMID: 12639547
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