GW583340 DIHYDROCHLORIDE

Definition

ChEBI: N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[2-[(2-methylsulfonylethylamino)methyl]-4-thiazolyl]-4-quinazolinamine is a member of quinazolines.

Biological Activity

Potent dual EGFR/ErbB2 tyrosine kinase inhibitor (IC 50 values are 0.01 and 0.014 μ M respectively). Selectively inhibits growth of human tumor cells overexpressing EGFR and ErbB2: IC 50 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. In vivo, inhibits tumor growth by ~ 80% in a murine xenograft model following oral administration.