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CGI1746 has exquisite selectivity for Btk and inhibits both auto- and transphosphorylation steps necessary for enzyme activation. CGI1746 blocks B cell receptor-dependent B cell proliferation and in prophylactic regimens reduces autoantibody levels in collagen-induced arthritis. CGI1746 decreases cytokine levels within joints and ameliorates disease. CGI1746 shows comparable efficacy to TNFα blockade and significantly reduces clinical scores, as well as joint inflammation, in mice or rats with established arthritis.
Brand: BCM
Target: IC50: 1.9 nM (Btk)
Solubility: Soluble in DMSO and Ethanol. Insoluble in Water.
Attribute [CAS No.] 910232-84-7 [Formula] C34H37N5O4 [Molecular] 579.69 [Chem Name] 4-(tert-Butyl)-N-(2-methyl-3-(4-methyl-6-((4-(morpholine-4-carbonyl)phenyl)amino)-5-oxo-4,5-dihydropyrazin-2-yl)phenyl)benzamide [Synonym] CGI1746; CGI-1746 [MDL No.] MFCD18782602 [Form] Solid
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