Table 1.
Antiproliferative activity of FGFR inhibitors on transformed Ba/F3 cells
| Ba/F3 cell lines | EC50, nM | |||||
| FIIN-1 | BGJ398 | FIIN-2 | FIIN-3 | FRIN-2 | FRIN-3 | |
| Parental | >3,300 | >3,300 | >3,300 | 2,970 | >3,300 | >3,300 |
| FGFR1 | 14 | 3 | 4 | 1 | ||
| FGFR2 | 7 | 4 | 1 | <1 | 10 | 3 |
| FGFR2 (V564M) | 1,000 | 1,500 | 58 | 64 | 2,810 | 1,380 |
| FGFR2 (V564F) | >3,300 | 3,145 | 100 | 71 | ||
| FGFR2 (E565K) | >3,300 | 490 | 273 | 69 | ||
| FGFR2 (K659N) | 3,710 | 25 | 9 | 6 | ||
| FGFR2 (M538I) | 839 | 43 | 27 | 30 | ||
| FGFR2 (C491A) | 168 | 1 | 8 | 3 | 195 | 26 |
| FGFR2(C491A/V564M) | >3,300 | 2,100 | 3,140 | 1,000 | ||
| FGFR3 (S249C) | 10 | 67 | 93 | 41 | ||
| FGFR4 | >1,000 | >1,000 | 32 | 22 | >1,000 | >1,000 |
| EGFR (VIII) | >3,300 | >3,300 | 506 | 135 | >3,300 | 1,840 |
| EGFR (L858R) | >3,300 | >3,300 | 231 | 16.8 | 2,590 | 2,538 |
| EGFR DEL(E746-A750) | 240 | |||||
| EGFR (T790M/L858R) | >3,300 | >3,300 | 1,773 | 231 | >3,300 | >3,300 |
| EGFR (DEL/T790M) | 687 | |||||
| EGFR (C797S/L858R) | >3,300 | >3,300 | >3,300 | |||