Table 3.
IC50 values for inhibition of ALK Y1604 phosphorylation by ceritinib or crizotinib in PC12 cells
| ALK mutation | Ceritinib (IC50 nM) | Normalized to IC50 of wt | Crizotinib (IC50 nM) | Normalized to IC50 of WT | Fold change |
|---|---|---|---|---|---|
| wt | 5.3 ± 0.2 | 1.0 | 17.8 ± 0.2 | 1 | 3.4 |
| G1128A | 19.8 ± 3.5 | 3.7 | 22.2 ± 3.4 | 1.2 | 1.1 |
| I1171N | 46.6 ± 16 | 8.8 | 139.5 ± 13.8 | 7.8 | 3.0 |
| F1174L | 16.9 ± 8 | 3.2 | 29.9 ± 4.8 | 1.7 | 1.8 |
| R1192P | 26.1 ± 1.2 | 4.9 | 28.1 ± 7.5 | 1.6 | 1.1 |
| F1245C | 24.6 ± 6.4 | 4.6 | 37.5 ± 7.7 | 2.1 | 1.5 |
| G1269A | 28.9 ± 3.6 | 5.5 | 113.5 ± 8.5 | 6.4 | 3.9 |
| R1275Q | 10.8 ± 3.5 | 2.0 | 30.3 ± 0.9 | 1.7 | 2.8 |
| Y1278S | 20.5 ± 0.1 | 3.9 | 69.5 ± 0.03 | 3.9 | 3.4 |
IC50 values were determined by quantification of Y1604 phosphorylation from the immunoblots in Supplemental Figure 1. Values represent mean ± SD from at least two independent experiments.