Table 1.
Activity of nilotinib and imatinib against kinases involved in the pathogenesis of GIST. IC50 values are presented as means.
| KIT mutation (cell lines) | Nilotinib IC50, nM | Imatinib IC50, nM | Reference |
|---|---|---|---|
| Exon 11 KITV560del (Ba/F3) | 26 | 27 | 20 |
| Exon 13 KITK462E (GIST882) | 160 | 120 | 20 |
| Exon 11 KITV560G (HMC-1560) | 108 | 74 | 55 |
| Exon 11/exon 13 KITV560del/V654A (Ba/F3) | 192 | 3927 | 33 |
| Exon 11/exon 17 KITV559D/D820Y (Ba/F3) | 297 | 3202 | 33 |
| PDGFRA + PDGFRB (A31) | 71a | 74a | 20 |
| PDGFRB (Tel Ba/F3) | 57 | 39 | 20 |
a
Data shown represent kinase autophosphorylation.