In Vitro: PT-262 (5-40 μM; 24 h) induces cytotoxicity and proliferation inhibition in human lung cancer cells. PT-262 (2-20 μM; 4-24 h) induces caspase-3 activation, mitochondrial dysfunction and apoptosis in lung cancer cells. PT-262 (10-20 μM; 24 h) induces the accumulation of G2/M phases in both the p53-wild type and p53-null lung cancer cells, and inhibits the phosphorylation of CDC2 proteins. PT-262 (0-10 μM; 24 h) represses ERK phosphorylation in lung cancer cells. PT-262 (2 μM; 24 h) induces the cytoskeleton alteration and cell elongation in lung carcinoma A549 cells. PT-262 (2-10 μM; 6 h) significantly blocks the cell migration in a concentration-dependent manner.