TABLE 2

Inhibition of cell proliferation by ErbB inhibitors


Cell Line (Receptor Overexpressed)

IC50
JNJ-28871063
Lapatinib
Gefitinib
Erlotinib
nM
N87 (HER2) 159 ± 23 13 ± 5 377 ± 125 2013 ± 102
BT474 (HER2) 60 ± 6 14 ± 5 487 ± 218 4890 ± 1039
SKBR3 (HER2) 168 ± 20 9 ± 1 1172 ± 257 5807 ± 847
A431 (EGFR) 702 ± 153 395 ± 156 825 ± 106 650 ± 118
HN5 (EGFR) 516 ± 76 42 ± 3 32 ± 5 41 ± 1
HeLa >10,000 >10,000 >10,000 >10,000
A375 >10,000 >10,000 >10,000 >10,000
HCT116 >10,000 >10,000 >10,000 >10,000
HT29 >10,000 2035 ± 271 4220 ± 459 9917 ± 61
MRC5 primary fibroblasts
>10,000
5671 ± 401
8795 ± 800
1864 ± 218