Table 2.

In vitro activity of selected compounds against KIT wild-type and distinct KIT mutants

In vitro activity of selected compounds against KIT wild-type and distinct KIT mutants

IC50 indicates the concentration for half-maximal inhibitory activity in vitro for proliferation/growth. NR indicates not reported.

*IC50 for in vitro experiments using BA/F3 cells stimulated with recombinant human stem cell factor only; when IL-3 was added, IC50 was 24360 nmol/L.

†IC50 for in vitro experiments using BA/F3 cells stimulated with recombinant human stem cell factor only; when IL-3 was added, IC50 was 345 nmol/L.

‡IC50 for inhibition of KIT kinase activity is indicated instead of the IC50 value for inhibition of proliferation.

§IC50 for experiments performed with HMC1.2 cell line harboring KITD816V and KITV560D mutations.

‖IC50 for the inhibition of KIT autophosphorylation in vitro is indicated instead of the IC50 value for inhibition of proliferation.

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