| Identification | Back Directory | [Name]
PRT-060318 | [CAS]
1194961-19-7 | [Synonyms]
PRT 318
CS-1688
P 142-76
PRT-060318
PRT-060318 ≥95%
PRT-060318(PRT318)
PRT 060318 ;PRT060318;PRT 318;PRT-318;PRT318
2-(((1R,2S)-2-aminocyclohexyl)amino)-4-(m-tolylamino)pyrimidine-5-carboxamide
2-[[(1R,2S)-2-Aminocyclohexyl]amino]-4-[(3-methylphenyl)amino]-5-pyrimidinecarboxamide
5-Pyrimidinecarboxamide, 2-[[(1R,2S)-2-aminocyclohexyl]amino]-4-[(3-methylphenyl)amino]- | [Molecular Formula]
C18H24N6O | [MDL Number]
MFCD28155088 | [MOL File]
1194961-19-7.mol | [Molecular Weight]
340.42 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 | [storage]
Store at -20°C | [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. |
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| Company Name: |
Tcichem, Inc.
|
| Tel: |
13918644899 |
| Website: |
http://www.is0513.com/ShowSupplierProductsList19113/0.htm |
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