Table 2.
Antiproliferative activity of FGFR inhibitors against various cancer cell lines
Cell line | Genotype | Cancer type | EC50, nM | ||||
BGJ398 | FIIN-2 | FIIN-3 | FRIN-2 | FRIN-3 | |||
H2077 | NSCLC | 7 | 3.9 | 5.3 | |||
H2077 (V561M) | FGFR1 amplification | Transgenic | >1,000 | 16.1 | 1.4 | ||
H2077 (vector) | 3.5 | 3.9 | 2.4 | ||||
H1581 | NSCLC | 10.5 | 4.8 | 2.5 | |||
H1581 (V561M) | FGFR1 amplification | Transgenic | 507.5 | 23.6 | 11.8 | ||
H1581 (vector) | 9 | 3.3 | 2.15 | ||||
H520 | FGFR1 amplification | NSCLC | 121.2 | 109.3 | 98.9 | ||
Kato III | FGFR2 amplification | Gastric carcinoma | 3.4 | 1.9 | 2.5 | ||
AN3 CA | FGFR2 N549K activating mutation | Endometrial adenocarcinoma | 26.6 | 23.9 | 26.2 | ||
RT112 | FGFR3/TACC3 fusion and FGFR3 amplification | Bladder carcinoma | 2.7 | 6.8 | 15.9 | ||
A2780 | FGFR4 amplification | Ovarian carcinoma | 0.5 | 0.04 | 0.01 | 3.2 | 0.6 |
4T1 | FGFRs amplification | Breast carcinoma | 125 | 23 | 46 | 455 | 669 |
SKOV-3 | FGFRs and EGFR amplification | Bladder carcinoma | 1,633 | 925 | 499 | 1,654 | 1,649 |