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Beschreibung

A cell-permeable quinazoline compound that acts as a potent and reversible CXCR4 antagonist (IC50 = 36.2 nM for SDF-1/CXCL12 binding to hCXCR4-transfected HEK293 membrane) with selectivity over closely related human chemokine receptors CXCR2, CCR2, CCR4 and CCR5 (IC50 >10 µ,M). Shown to inhibit CXCL12-induced Ca2+-mobilization and cell migration in hCXCR4-HEK293 cells (IC50 = 100.1 and 41 nM, respectively), and rapidly mobilize CXCR4+, CD34+ and CD133+ stem cells from bone marrow in C57BL/6 male mice (6 mg/kg, s.c).