CGI1746

CGI1746 is a potent, selective inhibitor of Bruton's tyrosine kinase (BTK, IC50 = 1.9 nM), a non-receptor tyrosine kinase that is important in B lymphocyte development. It blocks both auto-and trans-phosphorylation of BTK by occupying an SH3 binding pocket in the un-phosphorylated enzyme. CGI1746 prevents B-cell antigen receptor-mediated B lymphocyte proliferation and suppresses FCgammaRIII-induced TNFalpha, IL-1beta, and IL-6 production in macrophages. It reduces cytokine levels within joints and ameliorates symptoms in a mouse model of autoantibody-induced arthritis.Formal Name: N-[3-[4,5-dihydro-4-methyl-6-[[4-(4-morpholinylcarbonyl)phenyl]amino]-5-oxo-2-pyrazinyl]-2-methylphenyl]-4-(1,1-dimethylethyl)-benzamide. CAS Number: 910232-84-7. Molecular Formula: C34H37N5O4. Formula Weight: 579.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 25 mg/ml, DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml, Ethanol: 0.25 mg/ml. lambdamax: 234, 355 nm. SMILES: O=C(C1=CC=C(NC2=NC(C3=CC=CC(NC(C4=CC=C(C(C)(C)C)C=C4)=O)=C3C)=CN(C)C2=O)C=C1)N5CCOCC5. InChi Code: InChI=1S/C34H37N5O4/c1-22-27(7-6-8-28(22)37-31(40)23-9-13-25(14-10-23)34(2,3)4)29-21-38(5)33(42)30(36-29)35-26-15-11-24(12-16-26)32(41)39-17-19-43-20-18-39/h6-16,21H,17-20H2,1-5H3,(H,35,36)(H,37,40). InChi Key: JIFCFQDXHMUPGP-UHFFFAOYSA-N.