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.1 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).2 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.3 Plerixafor also increases T cell trafficking in mouse blood, spleen, and central nervous system.4,5 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.6
1.Hatse, S., Princen, K., Bridger, G., et al.Chemokine receptor inhibition by AMD3100 is strictly confined to CXCR4FEBS Lett.527(1-3)255-262(2002) 2.De Clercq, E., Yamamoto, N., Pauwels, R., et al.Highly potent and selective inhibition of human immunodeficiency virus by the bicyclam derivative JM3100Antimicrob. Agents Chemother.38(4)668-674(1994) 3.Hess, D.A., Bonde, J., Craft, T.C., et al.Human progenitor cells rapidly mobilized by AMD3100 repopulate NOD/SCID mice with increased frequency in comparison to cells from the same donor mobilized by granulocyte colony stimulating factorBiol. Blood Marrow Transplant13(4)398-411(2007) 4.Bernardini, G., SciumÈ, G., Bosisio, D., et al.CCL3 and CXCL12 regulate trafficking of mouse bone marrow NK cell subsetsBlood111(7)3626-3634(2008) 5.McCandless, E.E., Zhang, B., Diamond, M.S., et al.CXCR4 antagonism increases T cell trafficking in the central nervous system and improves survival from west nile virus encephalitisProc. Natl. Acad. Sci. U.S.A.105(32)11270-11275(2008) 6.Smith, M.C., Luker, K.E., Garbow, J.R., et al.CXCR4 regulates growth of both primary and metastatic breast cancerCancer Res.64(23)8604-8612(2004)