Table 1. Inhibition of KIT/PDGFRA autophosphorylation and proliferation in cell lines.
pKIT inhibition IC50 (nM)
Cell lineMutationExonTissueBLU-285ImatinibSunitinibRegorafenib
M-07eKIT WTHuman megakaryoblastic leukemia192336363
HMC1.1KIT V560G11Human mast cell leukemia10021138
KasumiKIT N822K17Human acute myeloid leukemia401296111
P815KIT D816Y17Murine mastocytoma221236611128
HMC1.2KIT V560G/D816V11/17Human mast cell leukemia4914414,488314
CHOPDGFRA WTEngineered95<100
CHOPDGFRA V561D12Engineered40<100
CHOPDGFRA D842V18Engineered303145
Proliferation IC50 (nM)
Cell lineKIT mutationExonTissueBLU-285ImatinibSunitinibRegorafenib
M-07eWTHuman megakaryoblastic leukemia417604132678
HMC1.1V560G11Human mast cell leukemia3443613115
KasumiN822K17Human acute myeloid leukemia7538231211
P815D816Y17Murine mastocytoma2022,8112301,974
HMC1.2V560G/D816V11/17Human mast cell leukemia12511,3551506>25,000