A Bi drug is derived from 2,6-pyridinedicarboxaldehyde bis(4N-methylthiosemicarbazone). The drug shows high anticancer activities against human lung cancer cells A549 and H460. No cytotoxicity is caused by the drug to normal human lung fibroblast (HLF) cell. The drug effectively inhibits A549 xenograft tumor growth on tumor-bearing mice. No harmful effect on mouse weight and liver is found after treatment with this drug.