Baricitinib (LY-3009104, INCB-028050)

Description: Baricitinib, (also known as LY3009104 or INCB028050; trade name: Olumiant), is a potent, selective, ATP competitive and orally bioavailable inhibitor of tyrosine-protein kinase JAK1 (Janus kinase) or JAK2 with anti-inflammatory activity. AS of May 2018, it was approved by FDA for the treatment of rheumatoid arthritis (RA) in the United States. In vitro, it is able to inhibit JAK1 and JAK2 with IC50 values in the low nanomolar range of 5.9 and 5.7 nM, respectively, while it displays low inhibitory activity for JAK3 and moderate activity for TYK2. Baricitinib inhibits intracellular signaling of several proinflammatory cytokines such as IL-6 and IL-23 at concentrations< 50 nM. JAK signaling is central to a number of fundamental processes including the generation of RBCs.

References: J Immunol. 2010 May 1; 184(9):5298-307; Curr Opin Pharmacol. 2012 Aug; 12(4):464-70.

Related CAS: 1187595-84-1 (phosphate); 1187594-09-7 (free base)