Table 1. Growth inhibition of tumor cell lines with activation of FGFR signaling by INCB054828.
| Cell Line (Histology) | FGFR Alteration | Mean GI50 ± S.D. (nM) |
|---|---|---|
| H1581 (lung cancer) | FGFR1 amplification | 14 ± 9 |
| DMS-114 (lung cancer) | FGFR1 amplification | 27 |
| KG1a (AML) | FGFR1OP2-FGFR1 fusion | 3 ± 1 |
| KATO III (gastric cancer) | FGFR2 amplification | 3 ± 1 |
| AN3CA (endometrial cancer) | FGFR2 N310R/N549K mutations | 48 ± 28 |
| RT-112 (bladder cancer) | FGFR3-TACC3 fusion | 7 ± 3 |
| RT-4 (bladder cancer) | FGFR3-TACC3 fusion | 12 |
| KMS-11 (myeloma) | IgH-FGFR3 translocation | 362 ± 282 |
| OPM-2 (myeloma) | IgH-FGFR3 translocation | 18 ± 9 |
| Engineered Cell Lines | ||
| Ba/F3-FGFR1-ZFN298 | FGFR1 fusion, 8P11 MPN | 0.9 ± 0.4 |
| Ba/F3-FGFR2-CCDC6 | FGFR2 fusion, cholangiocarcinoma | 1.2 ± 0.2 |
| Ba/F3-FGFR2-AHCYL | FGFR2 fusion, cholangiocarcinoma | 1.1 ± 0.3 |
MPN, myeloproliferative neoplasm