AS-604850

AS-604850是一种选择性ATP竞争性PI3Kγ抑制剂，对人类重组γ、.delta.、β和α亚型的IC50值分别为0.25、>20、>20和4.5µM。AS-604850抑制MCP-1介导的单核细胞趋化性，IC50值为21µM，并减少小鼠白细胞趋化性模型中RANTES诱导的腹膜中性粒细胞募集，ED50值为42.4mg/kg。AS-604850 is a selective, ATP-competitive inhibitor of PI3Kγ with IC50 values of 0.25, >20, >20, and 4.5 µM for the human recombinant γ, .delta., β, and α isoforms, respectively. AS-604850 inhibited MCP-1-mediated monocyte chemotaxis with an IC50 value of 21 µM and reduced RANTES-induced peritoneal neutrophil recruitment in a murine model of leukocyte chemotaxis with an ED50 value of 42.4 mg/kg.