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Table 2 Inhibition of the Activity of Wild-Type Kit and Primary Activating Kit Mutants by Motesanib and Imatinib*

From: Motesanib inhibits Kit mutations associated with gastrointestinal stromal tumors

 

IC50 of Kit Autophosphorylation, nM

IC50 of Stably Transfected Ba/F3 Cell Survival, nM

KIT Genotype

Motesanib

Imatinib

Motesanib

Imatinib

Wild-type

36

165

-

-

V560D

5

18

3

7

Δ552-559

1

5

0.4

1

AYins503-504

18

84

11

47

  1. *In autophosphorylation experiments, means from 2 experiments are shown, with the exception of Δ552-559, which was assessed once. Viability experiments were performed once.