中文名：PRT 060318
英文名：PRT 060318
纯度：≥99%
货号：P413822
Cas号：1194961-19-7
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
PRT-060318 2HCl PRT-060318 (PRT318) is a novel selective inhibitor of the Syk tyrosine kinase with an IC50 of 4 nM, as an approach to HIT treatment.
Targets
Syk (Cell-free assay) 4nM
In vitro
PRT318 inhibits platelet activation via GPVI/FcRγ, an ITAM receptor complex, but not via ADP or thrombin, which are G-protein coupled receptors. PRT318 effectively antagonizes CLL(chronic lymphocytic leukemia) cell survival after BCR triggering and in nurse-like cell-co-cultures. PRT318 inhibits Syk and extracellular signal-regulated kinase phosphorylation after BCR triggering.
In vivo
In both rabbit and pig models, intravenous infusion of PRT060318 targets maximal inhibition of Syk kinase activity and significantly inhibits arterial thrombosis. The antithrombotic activity of PRT060318 in pigs is remarkable because it was achieved with complete inhibition of CVXN-induced platelet aggregation, with no effect on ADP-induced platelet aggregation, and no prolongation of ear bleeding time. Also, Syk inhibitor PRT318 is an active agent in HIT. Inhibition of Syk signaling with the orally bio-available PRT318 limits the thrombocytopenic and thrombotic effects of HIT IC in vivo.
Cell Research(from reference)
Cell lines：LY3，LY4，LY7,LY18 cell lines
Concentrations：0-3μM
Incubation Time：0-72h
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关键字： 2-[[(1R,2S)-2-Aminocyclohexyl]amino]-4-[(3-methylphenyl)amino]-5-pyrimidinecarboxamide ; P 142-76 ; PRT 318
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