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A) Structures of known and newly synthesized cyclam-based CXCR4 inhibitors; B) Evaluation of surface CXCR4 expression in U87 cancer cell lines by flow cytometry. Grey, isotype; blue, U87, red, U87-stb-CXCR4; C) Inhibition binding assays of SDF1-Red (15 nM) with increasing concentrations of analyzed inhibitors, non-linear curve fit data is shown; D) tabulated IC50 and Ki values for analyzed CXCR4 inhibitors; reported at 95% confidence level.
