Table 1 The IC50 of FIIN-2, TAS-120 and PRN1371 to gatekeeper mutants of FGFRs.
From: Structural insights into the potency and selectivity of covalent pan-FGFR inhibitors
IC50, nM | ||||||||
|---|---|---|---|---|---|---|---|---|
kinase activity | FGFR1 | FGFR1 (V561M) | FGFR2 | FGFR2 (V564F) | FGFR3 | FGFR3 (V555M) | FGFR4 | FGFR4 (V550L) |
FIIN-2 | 6.4 | 216 | 2.9 | 276 | 6.7 | 97 | 21.0 | 255 |
TAS-120 | 7.8 | 224 | 2.7 | 52 | 2.1 | 110 | 12.1 | 90 |
PRN1371 | 2.5 | 84 | 4.1 | >1000 | 1.8 | 583 | 31.1 | >1000 |
