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| | PRT-060318 Basic information |
| Product Name: | PRT-060318 | | Synonyms: | PRT-060318;PRT-060318(PRT318);2-[[(1R,2S)-2-Aminocyclohexyl]amino]-4-[(3-methylphenyl)amino]-5-pyrimidinecarboxamide;P 142-76;PRT 318;2-(((1R,2S)-2-aminocyclohexyl)amino)-4-(m-tolylamino)pyrimidine-5-carboxamide;CS-1688;PRT-060318 ≥95% | | CAS: | 1194961-19-7 | | MF: | C18H24N6O | | MW: | 340.42 | | EINECS: | | | Product Categories: | | | Mol File: | 1194961-19-7.mol |  |
| | PRT-060318 Chemical Properties |
| Melting point | 152 - 155°C | | Boiling point | 602.1±65.0 °C(Predicted) | | density | 1.277±0.06 g/cm3(Predicted) | | storage temp. | Refrigerator, under inert atmosphere | | solubility | DMSO (Slightly), Methanol (Slightly) | | form | Solid | | pka | 14.10±0.50(Predicted) | | color | Pale Brown |
| | PRT-060318 Usage And Synthesis |
| Description | PRT060318 is a potent and selective inhibitor of spleen tyrosine kinase (Syk; IC50 = 4 nM). 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. 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. PRT060318 also inhibits CLL B cell chemotaxis and pseudoemperipolesis. | | Uses | PRT 060318 is a novel selective inhibitor of the tyrosine kinase Syk. PRT 060318 may be used in Heparin-Induced Thrombocytopenia (HIT) treatment. HIT is a major cause of morbidity and mortality. | | in vitro | 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 [1]. | | in vivo | animal study showed that in contrast to vehicle-treated mice developed the expected thrombocytopenia, prt-060318-treated mice had no significant change in platelet counts after injection of heparin. moreover, the nadir platelet counts of prt-060318-treated mice were found to be significantly higher than control mice. the prt-060318-treated mice showed no bleeding diathesis or other adverse effects. in addition, prt-060318 treatment in crush thrombosis model resulted in significant inhibition of platelet deposition without changing bleeding time [1]. | | IC 50 | 4 nm | | references | [1] reilly mp,sinha u,andré p,taylor sm,pak y,deguzman fr,nanda n,pandey a,stolla m,bergmeier w,mckenzie se. 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. |
| | PRT-060318 Preparation Products And Raw materials |
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