Potent dual EGFR/ErbB2 tyrosine kinase inhibitor (IC50
values are 0.01 and 0.014 μ
M respectively). Selectively inhibits growth of human tumor cells overexpressing EGFR and ErbB2 (IC50
values are 0.11 μ
M for inhibition of HN5, N87 and BT474 tumor cell lines vs. > 30 μ
M for inhibition of non-tumor cell line HFF). Inhibits tumor growth in vivo
by ~ 80% in a murine xenograft model following oral administration.
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.
Sold for research purposes under agreement from GlaxoSmithKline.
Discovery and biological evaluation of potent dual ErbB-2/EGFR tyrosine kinase inhibitors: 6-thiazolylquinazolines.
Gaul et al.