PRT060318

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.Formal Name: 2-[[(1R,2S)-2-aminocyclohexyl]amino]-4-[(3-methylphenyl)amino]-5-pyrimidinecarboxamide. CAS Number: 1194961-19-7. Synonyms: P142-76, PRT318. Molecular Formula: C18H24N6O. Formula Weight: 340.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3 mg/ml, DMF:PBS (pH7.2) (1:30): 0.03 mg/ml, DMSO: Insouble, Ethanol: Insouble, PBS (pH 7.2): Insouble. lambdamax: 250, 288 nm. SMILES: N[C@@H]1[C@H](NC2=NC=C(C(N)=O)C(NC3=CC(C)=CC=C3)=N2)CCCC1. 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. InChi Key: NZNTWOVDIXCHHS-LSDHHAIUSA-N.