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Background Information:
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.
Reference:
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 × 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.*The product, RN486, being offered is a free base, confirmed by a perfect, high-precision Quantitative Elemental Analysis. Chemietek is the original manufacturer of the product.
APIM050235: RN486 (RN-486)
CAS No.: 1242156-23-5.
Molecular Formula: C35H35FN6O3.
Molecular Weight: 606.7.
Purity: >99.5% (HPLC at 214 and 254 nm).
QC: HPLC-MS, 1HNMR and Quantitative Elemental Analysis*.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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