The invention provides an anti-tumor peptide molecule with multiplex targeting performance and selectivity and application thereof, and belongs to the field of targeted medicine molecules. The molecule structure completeness and the cell non-toxicity can be maintained in the normal cell positions; cell antipersonnel fragments can be released in the tumor cell positions, so that the selective killing on the tumor cells can be realized; meanwhile, the duplex targeting performance can be realized on the tumor cells. The peptide molecule has the following sequence of Ac-Arg-Gly-Asp-Gly-Pro-Leu-Gly-Leu-Ala-Gly-Ile-Ile-Ile-Gly-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-NH2(RR22), and can be subjected to enzymolysis by substrate metalloprotease to release LR15 fragments Leu-Ala-Gly-Ile-Ile-Ile-Gly-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-NH2 with the tumor cell killing performance. The anti-tumor peptide molecule provided by the invention can be used for preparing tumor cell selective killing agents, and can be effectively applied to targeted killing of tumor cells. Compared with other targeting medicine, the anti-tumor peptide molecule has wider application values.