GW583340 (dihydrochloride)

GW 583340 dihydrochloride is an orally active ErbB-2/EGFR tyrosine kinase inhibitor. GW 583340 dihydrochloride exhibits antitumor activity in xenograft models with EGFR overexpression or ErbB-2 overexpression. GW 583340 dihydrochloride is applicable to research related to head and neck cancer, breast cancer, and gastric cancer^[1]. In Vitro:GW583340 (compound 6) dihydrochloride potently inhibits purified EGFR and ErbB-2 tyrosine kinase activity in vitro cell-free assays, with an average dual enzyme inhibition IC₅₀ of 0.012 μM^[1].
GW583340 dihydrochloride potently and selectively inhibits the proliferation of EGFR-overexpressing HN5, ErbB-2-overexpressing N87, and ErbB-2-overexpressing BT474 human tumor cell lines, with an average tumor cell IC₅₀ of 0.11 μM and a selectivity ratio of >210-fold for tumor cells over normal HFF cells^[1]. In Vivo:GW583340 (compound 6) (30-100 mg/kg; p.o.; twice daily; 21 days) dihydrochloride produces 81% tumor inhibition in HN5 EGFR-overexpressing human head and neck carcinoma xenografts in female CD-1 mice^[1].
GW583340 (30-100 mg/kg; p.o.; twice daily; 21 days) dihydrochloride produces 83% tumor inhibition in BT474 ErbB-2-overexpressing human breast carcinoma xenografts in female CD-1 mice, with no significant body weight loss observed^[1].