Table 3. ARQ 087 activity in FGFR dysregulated cell lines.
Cancer | Cell Line | FGFR Status [ref.] | ARQ 087 GI50 μM |
---|---|---|---|
Colon | NCI-H716 | FGFR2 amp / FGFR2-COL14A1 fusion [44]/[45] | 0.10 |
Gastric | SNU-16 | FGFR2 amp / PDHX-FGFR2 fusion [11]/[45] | 0.10 |
Blood | KG-1 | FGFROP2-FGFR1 fusion [46] | 0.13 |
Gastric | KATO-III | Amplified FGFR2 [11] | 0.20 |
Ovarian | SKOV3 | Over expression FGFR4 [47] | 0.28 |
Bladder | J82 | FGFR3 5652E [48] | 0.30 |
Ovarian | A2780 | Over expression FGFR 4 [47] | 0.33 |
Leukemia | K-562 | Over expression FGFR3 / 4 [49] | 0.40 |
Breast | MFM-223 | Amplified FGFR2 [42] | 0.50 |
Bladder | RT112 | FGFR3-TACC3 fusion [19] | 0.65 |
Endometrial | MFE-280 | FGFR2 S252W [50] | 0.9 |
Endometrial | MFE-296 | FGFR2 N549K [50] | 1.0 |
Bladder | RT4 | FGFR3-TACC3 fusion [19] | 1.2 |
Bladder | SW-780 | FGFR3-BAIAP2L1 fusion [19] | 1.4 |
Endometrial | AN3CA | FGFR2 N549K [50] | 1.7 |