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.

KEYWORDS: RN486 | Supplier | BTK inhibitor | RN-486 | RN 486 | CT-RN486 | CAS [1242156-23-5] | B-Cell transformation | BTK | Inhibitor | Enzymes