产品描述:
Fenebrutinib is an inhibitor of Bruton’s tyrosine kinase (BTK; Kis = 0.91, 1.6, 1.3, 12.6, and 3.4 nM for wild-type BTK, BTKC481S, BTKC481R, BTKT474I, and BTKT474M, respectively).{63396} It is selective for BTK over a panel of 287 additional kinases at 1 µM. Fenebrutinib inhibits anti-IgM antibody-induced BTK phosphorylation in B cells (IC50 = 3.1 nM), as well as anti-IgM- or CD40L-induced proliferation of B cells (IC50s = 1.2 and 1.4 nM, respectively). In vivo, Fenebrutinib (0.06-16 mg/kg) reduces ankle thickness and cartilage damage in a rat model of collagen-induced arthritis.