Plerixafor-d4 is intended for use as an internal standard for the quantification of plerixafor by GC- or LC-MS. Plerixafor is a partial antagonist of chemokine receptor 4 (CXCR4) with IC50 values ranging from 0.02 to 0.13 μg/ml for inhibiting calcium flux in peripheral blood mononuclear cells (PBMCs), various types of T cells, and mouse lymphocytic leukemia cells. It is selective for CXCR4 over CXCR1-3 and CXCR5-9 (IC50s = >25 μg/ml). Plerixafor decreases infectious virus content in the supernatant of Jurkat cells chronically infected with HIV-1(IIIB) (EC50 = ~0.02 μg/ml). It rapidly mobilizes murine and human hematopoietic stem and murine long-term repopulating cells for transplantation alone and, with a synergistic effect, when used in combination with G-CSF. Plerixafor also increases T cell trafficking in mouse blood, spleen, and central nervous system. Plerixafor (1.25 mg/kg twice per day) decreases the number of 4T1 murine mammary carcinoma cells in the lung in a mouse model of lung metastasis.
Labelled Plerixafor, it is a hematopoietic stem cell (HSC) mobilizer that inhibits the CXCR4 chemokine receptor and blocks binding of its ligand, stromal cell-derived factor-1-α (SDF-1-α). This agent was approved on Dec. 15, 2008, as treatment in combination with granulocyte-colony stimulating factor (G-CSF) to mobilize HSCs to the peripheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin''s lymphoma (NHL) and multiple myeloma (MM).
