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GW 583340 dihydrochloride

Cat. No. 2239

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Chemical Name: N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[2-[[[2-(methylsulfonyl)ethyl]amino]methyl]-4-thiazolyl]-4-quinazolinamine dihydrochloride

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.

Technical Data

M.Wt:

671.03

Formula:

C₂₈H₂₅ClFN₅O₃S₂.2HCl

Solubility:

Soluble to 100 mM in DMSO with gentle warming

Purity:

>97 %

Storage:

Desiccate at +4°C

CAS No:

388082-81-3

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

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Safety Data Sheet: View Safety Data Sheet

References

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.

If you know of a relevant citation for this product please let us know.

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