WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406271
Description: PRT-060318, also known as PRT318 or P142–76, is a novel selective inhibitor of the tyrosine kinase Syk, as an approach to HIT treatment. PRT318 completely inhibited HIT immune complex-induced aggregation of both human and transgenic HIT mouse platelets. Transgenic HIT model mice were treated with KKO, a mouse monoclonal HIT-like antibody, and heparin. The experimental group received orally dosed PRT318, whereas the control group received vehicle. Nadir platelet counts of PRT318-treated mice were significantly higher than those of control mice. When examined with a novel thrombosis visualization technique, mice treated with PRT318 had significantly reduced thrombosis.
MedKoo Cat#: 406271
Chemical Formula: C18H24N6O
Exact Mass: 340.20116
Molecular Weight: 340.42
Elemental Analysis: C, 63.51; H, 7.11; N, 24.69; O, 4.70
Synonym: PRT060318; PRT 060318; PRT-060318; PRT318; PRT-318; PRT 318; P14-276.
IUPAC/Chemical Name: 2-(((1R,2S)-2-aminocyclohexyl)amino)-4-(m-tolylamino)pyrimidine-5-carboxamide
InChi Key: NZNTWOVDIXCHHS-LSDHHAIUSA-N
InChi Code: InChI=1S/C18H24N6O/c1-11-5-4-6-12(9-11)22-17-13(16(20)25)10-21-18(24-17)23-15-8-3-2-7-14(15)19/h4-6,9-10,14-15H,2-3,7-8,19H2,1H3,(H2,20,25)(H2,21,22,23,24)/t14-,15+/m0/s1
SMILES Code: O=C(C1=CN=C(N[C@H]2[C@@H](N)CCCC2)N=C1NC3=CC=CC(C)=C3)N
1: Nanì S, Fumagalli L, Sinha U, Kamen L, Scapini P, Berton G. Src family kinases and Syk are required for neutrophil extracellular trap formation in response to β-glucan particles. J Innate Immun. 2015;7(1):59-73. doi: 10.1159/000365249. Epub 2014 Sep 24. PubMed PMID: 25277753.
2: Cheng S, Guo A, Lu P, Ma J, Coleman M, Wang YL. Functional characterization of BTK(C481S) mutation that confers ibrutinib resistance: exploration of alternative kinase inhibitors. Leukemia. 2015 Apr;29(4):895-900. doi: 10.1038/leu.2014.263. Epub 2014 Sep 5. PubMed PMID: 25189416.
3: Hoellenriegel J, Coffey GP, Sinha U, Pandey A, Sivina M, Ferrajoli A, Ravandi F, Wierda WG, O'Brien S, Keating MJ, Burger JA. Selective, novel spleen tyrosine kinase (Syk) inhibitors suppress chronic lymphocytic leukemia B-cell activation and migration. Leukemia. 2012 Jul;26(7):1576-83. doi: 10.1038/leu.2012.24. Epub 2012 Feb 7. PubMed PMID: 22362000.
4: Andre P, Morooka T, Sim D, Abe K, Lowell C, Nanda N, Delaney S, Siu G, Yan Y, Hollenbach S, Pandey A, Gao H, Wang Y, Nakajima K, Parikh SA, Shi C, Phillips D, Owen W, Sinha U, Simon DI. Critical role for Syk in responses to vascular injury. Blood. 2011 Nov 3;118(18):5000-10. doi: 10.1182/blood-2011-06-360743. Epub 2011 Aug 31. PubMed PMID: 21881044; PubMed Central PMCID: PMC3208305.
5: 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. doi: 10.1182/blood-2010-03-274969. Epub 2010 Nov 18. PubMed PMID: 21088136; PubMed Central PMCID: PMC3568699.