产品描述:
PRT060318 is a potent and selective inhibitor of spleen tyrosine kinase (Syk; IC50 = 4 nM).{39127,39128} It is selective, inhibiting 92% of Syk activity, while other kinases retain >70% activity, at a concentration of 50 nM in a panel of 270 kinases.{39128} PRT060318 inhibits convulxin-induced aggregation of human platelet-rich plasma (IC50 = 2.5 μM) in vitro and prevents thrombosis in a transgenic mouse model of heparin-induced thrombocytopenia. It induces chronic lymphocytic leukemia (CLL) B cell apoptosis and inhibits the secretion of chemokines CCL3, CCL4, and CXCL13.{39219} PRT060318 also inhibits CLL B cell chemotaxis and pseudoemperipolesis.