Table 1.

Activity of ponatinib in a panel of FGFR-amplified or -mutated cancer cell lines

Phospho-FGFR IC50, nmol/LCell growth GI50, nmol/L
CancerCell lineFGFR status (ref.)PonatinibPonatinibDovitinibCediranibBIBF 1120Brivanib
EndometrialAN3CAFGFR2 N549K (16)41411240886>1,000
MFE-296FGFR2 N549K (16)361359210980>1,000
MFE-280aFGFR2 S252W (16)133535084258197
BladderMGH-U3FGFR3 Y375C (41)40b181204>1,000>1,000>1,000
UMUC14FGFR3 S249C (41–42)33b103182168625>1,000
GastricSNU16FGFR2 amp (43, 45)202599142473>1,000
KATO IIIFGFR2 amp (43)21106486233865
BreastMDA-MB-134FGFR1 amp (7)723186297226>1,000
SUM 52PEFGFR2 amp (8)6146376364>1,000
MFM-223FGFR2 amp (8)769411416>1,000>1,000
LungH1581FGFR1 amp (4)1332216168427>1,000
DMS-114FGFR1 amp (4)30108818911>1,000>1,000
H520FGFR1 amp (4)7155>1,000>1,000>1,000>1,000
ColonH716FGFR2 amp (14)973349178598

Abbreviations: amp, amplification; ref, reference for cell line FGFR genetic alteration and dependence for cell growth.

  • aTested in serum-free media plus FGF2.

  • bFRS2α phosphorylation.