Our study revealed that aaptamine blocked cell cycle progression to repress cell growth, to diminish clonogenicity and to attenuate cellular viability and invasive growth of NSCLC cells in which aaptamine dephosphorylated AKT and GSK3β in PI3K/AKT/GSK3β signalling cascades and targeted downstream cell cycle regulation drivers (CDK2/4 and Cyclin D1/E). This evidence concerns the gene CDK2 and non-small cell lung carcinoma.