Inhibition of wild type human GST-tagged HER2 (676 to end residues) expressed in baculovirus infected Sf9 cells incubated for 30 mins in presence of ATP by HTRF analysis
Inhibition of wild type human N-terminal GST tagged EGFR (669 to 1210 residues) expressed in Sf21 insect cells incubated for 30 mins in presence of ATP by HTRF analysis
Selectivity ratio of IC50 for wild type human N-terminal GST tagged EGFR (669 to 1210 residues) expressed in Sf21 insect cells to IC50 for wild type human GST-tagged HER2 (676 to end residues) expressed in baculovirus infected Sf9 cells
Toxicity in BALB/c nude mouse xenografted with human NCI-N87 cells assessed as reduction in body weight at 5 to 40 mg/kg, po administered once daily for 21 days
Antitumor activity against human NCI-N87 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition by measuring relative tumor growth at 20 mg/kg/day, po administered once daily for 21 days by caliper method relative to control
Antitumor activity against human NCI-N87 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition by measuring relative tumor growth at 10 mg/kg/day, po administered once daily for 21 days by caliper method relative to control
Potency index, ratio of test compound IC50 to neratinib IC50 for inhibition of wild type human GST-tagged HER2 (676 to end residues) expressed in baculovirus infected Sf9 cells incubated for 30 mins in presence of ATP by HTRF analysis
Potency index, ratio of test compound IC50 to pyrotinib IC50 for inhibition of wild type human GST-tagged HER2 (676 to end residues) expressed in baculovirus infected Sf9 cells incubated for 30 mins in presence of ATP by HTRF analysis
Antitumor activity against human NCI-N87 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition by measuring relative tumor growth at 5 mg/kg/day, po administered once daily for 21 days by caliper method relative to control
Metabolic stability in human liver microsomes assessed as intrinsic clearance at 1 uM preincubated for 5 mins followed by NADPH addition by LC-MS/MS analysis