Table 2.

Biochemical IC50 values for inhibition of kinase activity in cells expressing single mutation kinases

KinaseExonModelImatinibCrenolanibP
FIP1L1-PDGFRA12EOL-11 ± 0.221 ± 130.13
PDGFRA WTNoneCHO9 ± 411 ± 100.62
PDGFRA V561D12CHO32 ± 18319 ± 750.006a
PDGFRA N659K14CHO56 ± 3776 ± 670.77
PDGFRA RV560-561RERV14CHO5 ± 344 ± 190.11
PDGFRA D842V18CHO1,353 ± 3119 ± 3<0.001a
PDGFRA D842I18CHO>1,000124 ± 360.02a
PDGFRA D842Y18CHO388 ± 13788 ± 230.06
PDGFRA deletion DIMH842-84518CHO21 ± 323 ± 90.75
PDGFRA DI842-843IM18CHO781 ± 34210 ± 20.003a
PDGFRA deletion I84318CHO67 ± 43197 ± 710.12
PDGFRA deletion HDSN8455-848P18CHO266 ± 10587 ± 520.30
PDGFRA D846Y18CHO29 ± 1318 ± 60.67
PDGFRA N848K18CHO22 ± 739 ± 160.16
KIT exon 11 deletion11GIST-T18 ± 4>1,0000.05a
KIT D816V17CHO>1,000>1,0001.00
PDGFRA V561D12BaF313 ± 12134 ± 710.03a
PDGFRA D842V18BaF3272 ± 1632 ± 20.002a

NOTE: The values for crenolanib and imatinib represent the biochemical IC50 expressed in nmol/L units ± the SEM. Values represent the data from at least 3 replicate experiments per mutation.

  • aP < 0.05 by Wilcoxon rank sum test.