prt-060318-3hcl

Description: PRT-060318 3HCl (also known as PRT318 3HCl) is a novel, potent, selective inhibitor of the Syk tyrosine kinase, as an approach to HIT treatment. PRT-060318 was identified as a potent inhibitor of purified Syk kinase. Syk kinase was inhibited by 92%, while the activities all other kinases retained more than 70% when PRT-060318 were evaluated at a concentration of 50 nM in a broad panel of kinase enzyme assays. In addition, PRT-060318 could dose-responsively inhibited convulxin-induced human PRP aggregation. Moreover, it was found that PRT-060318 was able to dose-responsively inhibit the increases in intracellular calcium in convulxin-treated platelets.

References: Blood. 2011 Feb 17; 117(7): 2241-46; Leukemia. 2012 Jul; 26(7):1576-83; Blood. 2011 Nov 3; 118(18):5000-10.

Related CAS#:1194961-19-7 (free base)