Taken together, these results indicate that T22‐GFP‐H6‐FdU achieves selective biodistribution to tumor tissue and FdU delivery to target CXCR4+ cancer cells, as indicated by an enhancement in DNA damage and apoptotic tumor cell death, which triggers selective elimination of CXCR4+ cancer cells in vivo, achieving, therefore, targeted FdU delivery to target cancer cells. Here, CXCR4 is linked to neoplasm.