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Plerixafor (AMD3100) is a small-molecule antagonist of CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively [1].

CXCR4 and -1 are key factors in regulating cancer cell invasion and metastasis, and plerixafor can prevent the binding of -1 to CXCR4 for inhibiting cancer metastasis [2]. Plerixafor interfered with CXCL12/CXCR4 mediated retention of hematopoietic stem cells in the bone marrow, and resulted in their mobilization to the blood [3]. Plerixafor amplified the release of circulating neutrophils from the oriented area in the lung, while simultaneously preventing neutrophil returned to the bone marrow [4]. Three adults with WHIM syndrome were subcutaneously injected 0.01 to 0.02 mg/kg plerixafor twice daily for 6 months, circulating leukocytes were constantly increased, and associated with fewer infections [5].

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