Activity of ponatinib in a panel of FGFR-amplified or -mutated cancer cell lines
Phospho-FGFR IC50, nmol/L | Cell growth GI50, nmol/L | |||||||
---|---|---|---|---|---|---|---|---|
Cancer | Cell line | FGFR status (ref.) | Ponatinib | Ponatinib | Dovitinib | Cediranib | BIBF 1120 | Brivanib |
Endometrial | AN3CA | FGFR2 N549K (16) | 4 | 14 | 112 | 40 | 886 | >1,000 |
MFE-296 | FGFR2 N549K (16) | 3 | 61 | 359 | 210 | 980 | >1,000 | |
MFE-280a | FGFR2 S252W (16) | 13 | 35 | 350 | 84 | 258 | 197 | |
Bladder | MGH-U3 | FGFR3 Y375C (41) | 40b | 181 | 204 | >1,000 | >1,000 | >1,000 |
UMUC14 | FGFR3 S249C (41–42) | 33b | 103 | 182 | 168 | 625 | >1,000 | |
Gastric | SNU16 | FGFR2 amp (43, 45) | 20 | 25 | 99 | 142 | 473 | >1,000 |
KATO III | FGFR2 amp (43) | 21 | 10 | 64 | 86 | 233 | 865 | |
Breast | MDA-MB-134 | FGFR1 amp (7) | 7 | 23 | 186 | 297 | 226 | >1,000 |
SUM 52PE | FGFR2 amp (8) | 6 | 14 | 63 | 76 | 364 | >1,000 | |
MFM-223 | FGFR2 amp (8) | 7 | 69 | 411 | 416 | >1,000 | >1,000 | |
Lung | H1581 | FGFR1 amp (4) | 13 | 32 | 216 | 168 | 427 | >1,000 |
DMS-114 | FGFR1 amp (4) | 30 | 108 | 818 | 911 | >1,000 | >1,000 | |
H520 | FGFR1 amp (4) | 7 | 155 | >1,000 | >1,000 | >1,000 | >1,000 | |
Colon | H716 | FGFR2 amp (14) | 9 | 7 | 33 | 49 | 178 | 598 |