Motesanib inhibits Kit mutations associated with gastrointestinal stromal tumors

Table 3 Inhibition of the Activity of Kit Mutants Associated With Imatinib Resistance by Motesanib and Imatinib*

	IC₅₀ of Kit Autophosphorylation, nM		IC₅₀ of Stably Transfected Ba/F3 Cell Survival, nM
KIT Genotype	Motesanib	Imatinib	Motesanib	Imatinib
V560D/V654A	77	319	91	145
V560D/T670I	277	>3000	180	>3000
Y823D	64	>3000	62	330
D816V	>3000	>3000	-	-

*In autophosphorylation experiments, means from 2 experiments are shown, with the exception of V560D/V654A and D816V, which were assessed once. Viability experiments were performed once.

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