Inhibitory activity of BIBU1361 and BIBX1382 on the tyrosine kinase activity of various protein kinases
The IC50 values were generated from 11-point dose-response curves and are given in nanomolar concentration. The IC50 values were determined as described under Materials and Methods and confirmed in at least three independent experiments. The IC50 values for Iressa were determined for comparison.
Kinases | BIBU1361 | BIBX1382 | Iressa |
|---|---|---|---|
| EGFR | 3 | 3 | 4 |
| HER2 | 290 | 3400 | 1830 |
| IGF1R | >10,000 | >10,000 | >10,000 |
| β-InsRK | >10,000 | >10,000 | >10,000 |
| HGFR | >10,000 | >10,000 | >10,000 |
| c-src | >10,000 | >10,000 | >10,000 |
| VEGFR-2 | >10,000 | >10,000 | >10,000 |