AP-26113 exhibited approx 100-fold selectivity for ALK-positive lines compared with a approx 10-fold selectivity for PF-1066. At the highest doses tested, strong regressions were
achieved with AP-26113, but not PF-1066 .AP-26113 inhibited the tumor growth at 25 mg/kg in ALCL and at 10 mg/kg in NSCLC models [1]. AP26113 inhibits cell growth with IC50 of 11 nM and 16 nM in
Ba/F3 line (native EML4-ALK) and Ba/F3 line (EML4-ALK G1269S mutants). AP26113 inhibits ALK phosphorylationh with IC50 of 74 nM and 335 nM in Ba/F3 line (native EML4-ALK) and Ba/F3 line (EML4-ALK
E1210K mutants). AP26113 (10 mg/kg-75 mg/kg) is efficacious in PF-02341066-resistant EML4-ALK mutant mouse xenograft models.