PF-06463922 is more effective than crizotinib in inhibiting NIH-3T3 cell transformation by mutated ALK variants. Inhibition of NIH-3T3 cell transformation in focus-formation assays is shown for transfections with ALK harboring: (A) the R1275Q mutation, (B) the F1174L mutation, and (C) the F1245C mutation. The individual inhibition curves are shown for 3–4 experiments in each case for both crizotinib (blue dashed curves) and PF-06463922 (red solid curves), with data points from all experiments superimposed on the plots. Mean IC50 values (± SD) for crizotinib and PF-06463922 respectively were 7.5 nM and 0.6 nM for F1275Q, 23.2 nM and 2.8 nM for F1174L, and 13.8 nM and 3.0 nM for F1245C.