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CXCR4 probe 1 (compound 5) is a potent and specific CXCR4-targeted PET tracer that acts on the CXCR4-specific antagonist TN14003 (IC50: 6.9 nM). The CXCR4 probe 1 has potential as a CXCR4-specific imaging probe for the diagnosis and prognostic monitoring of inflammatory diseases, CXCR4-positive tumours and metastatic tumours.