Pricing updated 2019-04-24. Prices are subject to change without notice.
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.1,2 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 FCγRIII-induced TNFα, IL-1β, and IL-6 production in macrophages.1 It reduces cytokine levels within joints and ameliorates symptoms in a mouse model of autoantibody-induced arthritis.1
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di Paolo, J.A., Huang, T., Balazs, M., et al. Specific Btk inhibition suppresses B cell-
2. Akinleye, A., Chen, Y., Mukhi, N., et al. Ibrutinib and novel BTK inhibitors in clinical development J. Hematol. Oncol. 6(59), (2013).