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Description: LY2510924, a small cyclic peptide, is a novel, potent and selective CXCR4 (CXC chemokine receptor 4) antagonist that blocks SDF-1 binding to CXCR4 with an IC50 of 0.079 nM. As an inhibitor of CXC chemokine receptor 4 (CXCR4), LY2510924 has potential antineoplastic activity. CXCR4 inhibitor LY2510924 binds to the chemokine receptor CXCR4 upon subcutaneous administration, thereby preventing CXCR4 binding to its ligand, stromal derived factor-1 (SDF-1), and subsequent receptor activation. This may result in decreased tumor cell proliferation and migration. CXCR4, a chemokine receptor belonging to the G protein-coupled receptor (GPCR) gene family, plays an important role in chemotaxis and angiogenesis and is upregulated in several tumor cell types.
References: Mol Cancer Ther. 2015 Feb; 14(2):480-90.; Blood. 2015 Jul 9; 126(2):222-32.
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