RN486 (RN-486)

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: C₃₅H₃₅FN₆O_3.
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.