FC131 TFA

C-X-C chemokine receptor 4 (CXCR4) is a receptor for the stromal cell-derived factor-1 (SDF-1) which is designated as chemokine ligand 12 (CXCL12). It is involved in cell progression, hematopoiesis, cancer, HIV entry, and rheumatoid arthritis.^1,2,3 FC 131 is an inhibitor of CXCR4 activation by SDF-1 (IC₅₀ = 4.5 nM) and also blocks HIV-induced cytopathogenicity (EC₅₀ = 73 nM).³ FC 131 derivatives can be used for imaging CXCR4 and elucidating its function.⁴

1.Broxmeyer, H.E., Orschell, C.M., Clapp, D.W., et al.Rapid mobilization of murine and human hematopoietic stem and progenitor cells with AMD3100, a CXCR4 antagonistJ. Exp. Med.201(8)1307-1318(2005) 2.Dorsam, R.T., and Gutkind, J.S.G-protein-coupled receptors and cancerNat. Rev. Cancer7(2)79-94(2007) 3.Tamamura, H., Hiramatsu, K., Ueda, S., et al.Stereoselective synthesis of [L-Arg-L/D-3-(2-naphthyl)alanine]-type (E)-alkene dipeptide isosteres and its application to the synthesis and biological evaluation of pseudopeptide analogues of the CXCR4 antagonist FC131J. Med. Chem.48(2)380-391(2005) 4.Kuil, J., Buckle, T., and van Leeuwen, F.W.B.Imaging agents for the chemokine receptor 4 (CXCR4)Chem. Soc. Rev.41(15)5239-5261(2012)