Table 2.

Biochemical IC50 values for inhibition of PDGFRA kinase activity in transfected cells

1° Mutation2° MutationImatinibSorafenibSunitinib
WTNone<100<100<100
V561DNone<100<100<100
V561DD842V3,1003,100>1,000
Del DIMH842-845None<100<100ND
D842VNone1,7001,280>1,000

NOTE: The values for imatinib, sorafenib, and sunitinib represent the biochemical IC50 expressed in nmol/L units for the listed single mutant or compound mutant kinases. WT indicates the results for wild-type (unmutated), PDGF-AA ligand-stimulated PDGFRA kinase. The IC50 values for imatinib and sorafenib are from direct head-to-head comparisons from a minimum of 3 replicate experiments. The IC50 values for sunitinib are from a previous publication from our group (6). The IC50 for imatinib was not significantly different than the IC50 for sorafenib for any of these mutant kinases.

Abbreviation: ND, not determined.