Table 7.
IC50 values in purified EGFR, EGFR mutated, HER2, and HER4 kinases.
| Inhibitor | EGFR Wild-Type |
EGFR L858R |
EGFR D746–750 |
HER2 | HER4 |
|---|---|---|---|---|---|
| PD153035 | 29 ± 5.1 pM | 2.3 µM | |||
| Gefitinib | 33 nM [114] 3 nM [20,115] |
0.8 nM [20] |
3.7–10 µM [114] 1.83 µM [20] 343 nM [115] |
476 nM [115] |
|
| Erlotinib | 0.56 nM [115] 0.25 nM [116] |
0.36 nM [116] |
0.41 nM [116] |
512 nM [115] 22 nM [116] |
790 nM [115] 265 nM [116] |
| Afatinib | 0.5 nM [20] | 0.4 nM [20] | 14 nM [20] | ||
| Osimertinib | 1.2 nM [116] | 2.1 nM [116] | 1.2 nM [116] | 1.69 nM [116] | 3.06 nM [116] |