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GW 583340 dihydrochloride
Biological Activity for GW 583340 dihydrochloride
GW 583340 dihydrochloride is a 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.
Sold for research purposes under agreement from GlaxoSmithKline.
Compound Libraries for GW 583340 dihydrochloride
Technical Data for GW 583340 dihydrochloride
|Storage||Desiccate at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for GW 583340 dihydrochloride
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|DMSO||67.1||100 with gentle warming|
Preparing Stock Solutions for GW 583340 dihydrochloride
The following data is based on the product molecular weight 671.03. Batch specific molecular weights may vary from batch to batch due to the degree 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|
Product Datasheets for GW 583340 dihydrochloride
References for GW 583340 dihydrochloride
References are publications that support the biological activity of the product.
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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1 Citation for GW 583340 dihydrochloride
Citations are publications that use Tocris products. Selected citations for GW 583340 dihydrochloride include:
Sodani et al (2012) GW583340 and GW2974, human EGFR and HER-2 inhibitors, reverse ABCG2- and ABCB1-mediated drug resistance. Biochem Pharmacol 83 1613 PMID: 22414725
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