产品描述:
SCH 527123 is an allosteric antagonist of C-X-C chemokine receptor type 1 (CXCR1; IC50 = 43 nM in Ba/F3 cells) and CXCR2 (IC50 = 0.97 nM in HTS cells).{45387} It inhibits calcium flux induced by CXCL8 in Ba/F3 cells expressing human recombinant CXCR1 or CXCR2. SCH 527123 (3 nM) inhibits CXCL8-induced chemotaxis of Ba/F3 cells expressing human recombinant CXCR2 and CXCL1-induced chemotaxis of isolated human polymorphonuclear cells (PMNs). It also inhibits LPS-induced neutrophil infiltration into the lung (ED50 = 1.8 mg/kg) and increases mucin levels in bronchoalveolar lavage fluid (BALF) in a rat model of airway inflammation.{45388} SCH 527123 inhibits proliferation of wild-type (IC50s = 28.95 and 18.78 µM, respectively) and IL-8 overexpressing HCT116 and Caco-2 cells (IC50s = 39.45 and 25.45 µM, respectively).{45389} It reduces tumor growth in an HCT116 mouse xenograft model when administered at a dose of 50 mg/kg per day.