Table 2.

Inhibitory concentration of various TKIs against KIT and PDGFR imatinib-resistant mutants

MutantsReceptorSorafenib (nmol/L)Dasatinib (nmol/L)PKC412 (nmol/L)EXEL-0862 (nmol/L)SU-11248 (nmol/L)
GatekeeperKIT6010,000 (26)100 (35)Not reported70 (33)
PDGFR110Not reported50 (15)Not reportedNot reported
Activation loopKIT3,8001-100 (26)44 (27)42 (28)Not reported
PDGFR1,170Not reported50 (39)Not reported>1,000 (34)