Table 1.
In vitro inhibitory activity of BIBW2992
| BIBW2992 | Lapatinib | Canertinib | Gefitinib | |
|---|---|---|---|---|
| EGFRwt | 0.5 | 3 | 0.3 | 3 |
| EGFRL858R | 0.4 | 8 | 0.4 | 0.8 |
| EGFRL858R/T790M | 10 | >4000 | 26 | 1013 |
| HER2 | 14 | 15 | 30 | 1830 |
| β-InsRK | >100 000 | >100 000 | >100 000 | >100 000 |
| HGFR | 13 000 | >20 000 | >20 000 | >20 000 |
| c-SRC | >4000 | >20 000 | 1480 | >10 000 |
| VEGFR-2 | >100 000 | >100 000 | 24 900 | >100 000 |
Inhibitory activities of BIBW2992, lapatinib, canertinib and gefitinib on the tyrosine kinase activity of various protein kinases. The IC50 values were determined as described in ‘Materials and methods’, confirmed in independent experiments and are reported here as nM values.