Inhibitory potencies of ceritinib on human ectonucleotidases*
| Enzyme | IC50 ± SEM (µM) (or % inhibition at 50 µM) |
| Human umbilical cord membrane preparations with high CD39 expression | 11.3±0.8 |
| Recombinant human CD39 | 13.7±0.6 (Ki=11.0±0.6)† |
| NTPDase2 | >>50 (–8) |
| NTPDase3 | 22.7±4.0 |
| NTPDase8 | 20.3±1.5 |
| Soluble CD73 | >50 (33) |
| Membrane-bound CD73 | >50 (30) |
| NPP1 | >>50 (8) |
| NPP3 | >>50 (1) |
| NPP4 | >50 (15) |
| NPP5 | >>50 (1) |
| CD38 | >50 (19) |
*In all cases, three independent experiments were performed. Details on the assays can be found in the Methods Section.
†Determined by non-linear regression of the Michaelis-Menten plot data (see figure 4).
NPP, nucleotide pyrophosphatase/phosphodiesterase; NTPDase, nucleoside triphosphate diphosphohydrolase.