| Name | PRT-060318 |
| Description | PRT-060318 (P142-76) is a novel selective inhibitor of the Syk tyrosine kinase, as an approach to HIT treatment. |
| Cell Research | The numbers of cells treated with various doses of PRT318 are followed over time. PRT318 inhibits growth of the sensitive cell lines in a dose-dependent manner. Two sensitive (LY7 and LY18) and 2 resistant (LY3 and LY4) cell lines are treated with indicated doses of PRT318. (Only for Reference) |
| 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[1]. 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[2]. |
| 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[3]. 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[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : 5.6 mg/mL (16.45 mM), Sonication and heating are recommended.
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| Keywords | Syk | PRT-318 | PRT-060318 | PRT060318 | PRT 318 | PRT 060318 |
| Inhibitors Related | URMC-099 | Fostamatinib | Entospletinib | Ellagic acid | TC-S 7003 | Piceatannol | Cerdulatinib | ANTHRAQUINONE-2-CARBOXYLIC ACID | GSK1904529A | R406 | Gusacitinib | Cerdulatinib hydrochloride |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Angiogenesis related Compound Library | Post-Translational Modification Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Preclinical Compound Library |
United States
