RN486

RN486 is a selective, and reversible inhibitor of Bruton's tyrosine kinase (BTK), binding to the enzyme potently and competitively with an in vitro IC50 of 4.0 nM (enzymatic assay), and 0.3 nM (FRET binding assay). Highly selective over almost all other kinases including Syk and JAK, two validated RA (Rheumatoid Arthritis) targets. It exhibits an excellent pharmacokinetic profile, and displayed strong functional as well as disease-related activities by inhibiting immune responses mediated by two important immunoreceptors, BCR and FcR, in both human cells and rodents, producing dose dependent efficacy in both CIA and AIA, with evidence for substantial efficacy in combination with low-dose methotrexate.

Store at 0° C (short term), -20° C (long term), desiccated

HPLC-MS, ¹HNMR and Quantitative Elemental Analysis

1. D. Xu, et al, RN486, a selective Bruton's tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents. J Pharmacol Exp Ther. 2012 Apr; 341(1):90-103.

2. P. Mina-Osorio, et al, Suppression of glomerulonephritis in lupus-prone NZB x NZW mice by RN486, a selective inhibitor of Bruton's tyrosine kinase, Arthritis Rheum. 2013 Sep; 65(9):2380-91. doi: 10.1002/art.38047.