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. 2016 Apr 11;7(20):29131–29142. doi: 10.18632/oncotarget.8675

Figure 1. A674563 selectively inhibits FLT3-ITD.

Figure 1

(A) Anti-proliferation effects of AKT inhibitors (A674563, AZD5363, CCT128930, GDC0068, GSK690693, MK2206) and FLT3 inhibitors (TCS359, AC220) against FLT3-ITD positive AML cell lines (MOLM13, MOLM14, MV4-11) and FLT3 wt cell lines (U937, NB4, HL-60, PF-382 and SKM-1). (B) Inhibitory Effects of A674563 against auto-phosphorylation of FLT3 wt/mt kinases in the FLT3 wt/mt transformed BaF3 isogenic cell lines. (C) Biochemical IC50 determination of A674563 in ADP-Glo assay with purified FLT3-wt (kinase domain) and FLT3-ITD (ITD+kinase domain) proteins. (D) Kinetics study with purified FLT3 wt/ITD protein against a range of ATP concentrations. (E, F) Molecular modeling illustration of A674563 binding mode in AKT (homology model built upon PDB ID: 1RJB,) and FLT3 (PDB ID: 3CQU) kinases.