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. 2017 Nov 15;8(67):111110–111118. doi: 10.18632/oncotarget.22624

Figure 1. Characterization of CHMFL-KIT-031 as a KIT-V559D selective inhibitor.

Figure 1

(A) Chemical structure of CHMFL-KIT-031. (B) EC50 of CHMFL-KIT-031 for inhibition of auto-phosphorylation at KIT Y703, Y719 and Y823 sites on a panel of KIT mutants transformed BaF3 cells. (C) Kinomewide selectivity profiling of CHMFL-KIT-031 with KINOMEScan technology. (D) Schematic illustration of selectivity profile of CHMFL-KIT-031, Imatinib and Suninitib on the juxtamembrane domain primary mutants, ATP binding pocket secondary mutants and activation loop secondary mutants.