Fig. 3.
Inhibition of constitutive autophosphorylation of ITD-mutated FLT3 by SU5416 and SU5614.
MV 4-11 (FLT3 ITD) cells were incubated with varying concentrations of inhibitor and stimulated with recombinant human FL. Ligand-independent constitutive autophosphorylation was demonstrated (first 2 lanes), consistent with an activating mutation of FLT3. FLT3 autophosphorylation was ablated by treatment with SU5416 and SU5614 with an IC50 of 100 nM and 10 nM, respectively. The membrane was stripped and reprobed with an antibody to FLT3. FLT3 expression was unaffected by treatment with either inhibitor.
