The developed vMIP‐II‐TAT‐I peptide, incorporating a CXCR4‐targeted penetrating motif, demonstrated superior cellular uptake, with mean fluorescence intensity (MFI) 7.2‐fold higher in CXCR4‐positive AML cells and exhibited a high selectivity index (SI) for AML cells, with minimal impact on normal human hematopoietic stem cells (HSCs). This evidence concerns the gene CXCR4 and acute myeloid leukemia.