PRT-060318 (PRT318) dihydrochloride is a potent, selective and orally active tyrosine kinase Syk inhibitor with an IC50 of 3 nM. PRT-060318 dihydrochloride suppresses chronic lymphocytic leukemia (CLL) B cell activation and migration, and induces apoptosis. PRT-060318 dihydrochloride prevents Heparin -induced thrombocytopenia and thrombosis in a transgenic mouse model. PRT-060318 dihydrochloride can be used for CLL and thrombus research [1] [2].
In Vivo, PRT-060318 (PRT318) (10 and 30 mg/kg, i.g., b.i.d. for 7 days) dihydrochloride prevents heparin-induced thrombocytopenia and thrombosis in a transgenic mouse model[1].
In Vitro, PRT-060318 (PRT318) (0-3 µM, 15 min) dihydrochloride completely inhibits Heparin-induced thrombocytopenia (HIT) immune complex-induced aggregation of both human and transgenic HIT mouse platelets[1].
References:
[1]. Reilly MP, et al. PRT-060318, a novel Syk inhibitor, prevents heparin-induced thrombocytopenia and thrombosis in a transgenic mouse model. Blood. 2011 Feb 17;117(7):2241-6.
[2]. Hoellenriegel J, et al. Selective, novel spleen tyrosine kinase (Syk) inhibitors suppress chronic lymphocytic leukemia B-cell activation and migration. Leukemia. 2012 Jul;26(7):1576-83.
In Vivo, PRT-060318 (PRT318) (10 and 30 mg/kg, i.g., b.i.d. for 7 days) dihydrochloride prevents heparin-induced thrombocytopenia and thrombosis in a transgenic mouse model[1].
In Vitro, PRT-060318 (PRT318) (0-3 µM, 15 min) dihydrochloride completely inhibits Heparin-induced thrombocytopenia (HIT) immune complex-induced aggregation of both human and transgenic HIT mouse platelets[1].
References:
[1]. Reilly MP, et al. PRT-060318, a novel Syk inhibitor, prevents heparin-induced thrombocytopenia and thrombosis in a transgenic mouse model. Blood. 2011 Feb 17;117(7):2241-6.
[2]. Hoellenriegel J, et al. Selective, novel spleen tyrosine kinase (Syk) inhibitors suppress chronic lymphocytic leukemia B-cell activation and migration. Leukemia. 2012 Jul;26(7):1576-83.