Table 2.

In vitro cytotoxicity and ERK inactivation values in A375-VR cellsa

DrugTargetCytotoxicity IC50 (nmol/L)bp-ERK EC50 (nmol/L)c
GanetespibHsp901943
PLX-4720BRAF>10,000>10,000
GDC-0879BRAF>10,000>10,000
PF-562271FAK2,692865
LapatinibHER2, EGFR>10,000>10,000
AS703026MEK84
AZD6244MEK5126
TAK-733MEK916
CrizotinibMET, ALK1,734>10,000
CrenolanibPDGFR2,1743,338
EnzastaurinPKCβ5,717>10,000
VX-745p38>10,000>10,000
DasatinibSrc, Abl4,697>10,000
FostamatinibSyk>10,000>10,000
TivozanibVEGFR, PDGFR, c-Kit>10,000>10,000
SorafenibVEGFR, PDGFR, RAFs3,4814,819

Abbreviations: EGFR, EGF receptor; PDGFR, platelet-derived growth factor receptor; VEGFR, VEGF receptor.

  • aA375-VR cells were maintained in 5 μmol/L vemurafenib throughout the assay.

  • bIC50 values determined at 72 hours.

  • cEC50 values determined at 24 hours.