Table 1.
Targets of sorafenib in cell-free assays
Kinase | IC50 |
---|---|
CRAF | < 10nM |
mVEGFR3 | 10–20 nM |
mPDGFR, BRAF, BRAFV600E | 20–40 nM |
Flt-3, c-KIT | 40–80 nM |
VEGFR2 | 80–160 nM |
MEK, ERK, EGFR, HER-2 | Inactive at 10 000 nM |
Abbreviations: EGFR, epidermal growth factor receptor; ERK, extracellular signal-mediated kinase; Flt-3, fetal liver tyrosine kinase 3; HER-2, human epidermal growth factor receptor 2; IC50, concentration of drug required to cause 50% inhibition of an enzyme; m, murine; MEK, mitogen-activated protein kinase kinase; PDGFR, platelet-derived growth factor receptor; VEGFR, vascular endothelial growth factor receptor.