GW 583340 dihydrochloride

Cat. No. 2239

GW 583340 dihydrochloride C28H25ClFN5O3S2.2HCl [1173023-85-2]

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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:
1173023-85-2

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
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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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