Figure 1. CM-118 is a potent and selective dual inhibitor of c-Met and ALK. (A) CM-118 chemical structure is shown. (B) c-Met, ALK enzyme assays via HTRF; dose curves and mean IC₅₀ values are shown. (C) One micromole per liter racemic mixture of CM-118 and crizotinib (PF-1066) were assayed in 96 human kinases (KINOMEscan™). Kinase inhibition dendrograms are shown; the size of red dots is proportional to the degree of inhibition. (D) Serum-starved A549 cells were stimulated by HGF with vehicle or CM-118, then immunoblotted. (E) HGF-induced A549 cell migration was assayed without or with CM-118; left, crystal violet staining of migrated cells; right, migrated cells were quantified by 5 visual fields per filter. (F) HEK293 transiently expressing the indicated ALK constructs, treated with CM-118 for 6 h then immunoblotted. The phospho-ALK levels were quantified. CM-118 IC₅₀ (μmol/L) values are shown.