Pricing updated 2019-07-18. Prices are subject to change without notice.
CP 690,550 is a potent, cell-permeable inhibitor of all JAK isoforms (IC50s = 6.1, 12, and 8 nM for JAK1, JAK2, and JAK3, respectively).1 It is selective for JAK1-3 over ROCK-II and Lck (IC50s = 3,400 and 3,870 nM, respectively) as well as 28 additional kinases in enzyme assays (IC50s = >10,000 nM). It inhibits IL-2-mediated phosphorylation of JAK3 and STAT5 when used at a concentration of 30 ng/ml.2 CP 690,550 prevents rejection and prolongs survival in murine and cynomolgus monkey models of heterotopic heart and kidney transplantation, respectively. Formulations containing CP 690,550 have been used in the prevention of organ allograft rejection as well as in the treatment of the inflammatory or autoimmune components of a host of diseases, including rheumatoid arthritis and ulcerative colitis.2,3,4,5
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Haan, C., Rolvering, C., Raulf, F., et al. Jak1 has a dominant role over Jak3 in signal transduction through γc-
2. Changelian, P.S., Flanagan, M.E., Ball, D.J., et al. Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor Science 302(5646), 875-878 (2003).
Flanagan, M.E., Blumenkopf, T.A., Brissette, W.H., et al. Discovery of CP-
4. Cutolo, M. The kinase inhibitor tofacitinib in patients with rheumatoid arthritis: Latest findings and clinical potential Ther. Adv. Musculoskelet. Dis. 5(1), 3-11 (2013).
5. Sandborn, W.J., Ghosh, S., Panes, J., et al. Tofacitinib, an oral Janus kinase inhibitor, in active ulcerative colitis N. Engl. J. Med. 367(7), 616-624 (2012).
West, C.E., and Silverman, N. p38b and JAK-