Overall, the NGR-SSL-CA4 prepared in the present research has great potential in the multi-targeting therapy of glioma targeting the U87-MG cells, the VM formed by U87-MG cells as well as endothelial cells producing anti-U87-MG cells, anti-VM formed by U87-MG cells as well as anti-endothelial cell activity. The gene discussed is CA4; the disease is central nervous system cancer.