RN486

RN486 is a potent, selective and orally active Btk inhibitor with an IC50 of 4.0 nM and a Kd of 0.31 nM. RN486 is less active for other kinases. RN486 can be used for rheumatoid arthritis and systemic lupus erythematosus research[1][2][3].

Product Specifications

CAS Number

[1242156-23-5]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Btk

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/RN486.html

Purity

99.54

Solubility

DMSO : 24 mg/mL (ultrasonic; warming)

Smiles

O=C1C(NC2=CC=C(N3CCN(C)CC3)C=N2)=CC(C4=CC=CC(N5C=CC(C=C(C6CC6)C=C7F)=C7C5=O)=C4CO)=CN1C

Molecular Formula

C35H35FN6O3

Molecular Weight

606.69

Precautions

H302, H315, H319, H335

References & Citations

[1]Xu D, 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]Hsu J, et al. Bruton's Tyrosine Kinase mediates platelet receptor-induced generation of microparticles: a potential mechanism for amplification of inflammatory responses in rheumatoid arthritis synovial joints. Immunol Lett. 2013 Feb;150 (1-2) :97-104.|[3]Mina-Osorio P, 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.