The NCI-H460 cell line and its drug-resistant sublines may serve as sound models for cancer pharmacology research as they are likely to possess clinically relevant characters such as drug resistance both in vitro and in vivo. Our results also supported that the NCI-H460/TPT10 cell line could be a favorable model for studying TPT resistance, ABCG2-mediated MDR, and pharmacological evaluations on potential MDR reversal agents. The gene discussed is ABCG2; the disease is cancer.