BMS-986142

BMS-986142 is a potent and highly selective reversible inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 of 0.5 nM.

Product Specifications

CAS Number

[1643368-58-4]

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/BMS-986142.html

Purity

99.38

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

O=C1C2=C(C(F)=CC=C2)N(C)C(N1C3=C([C@]([C@]4=C(F)C=C(C(N)=O)C5=C4C6=C(C[C@@H](C(C)(C)O)CC6)N5)=CC=C3)C)=O

Molecular Formula

C32H30F2N4O4

Molecular Weight

572.60

Precautions

H302, H315, H319, H335

References & Citations

[1]Watterson SH, et al. Discovery of 6-Fluoro-5- (R) - (3- (S) - (8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3 (4H) -yl) -2-methylphenyl) -2- (S) - (2-hydroxypropan-2-yl) -2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142) : A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers. J Med Chem. 2016 Oct 13;59 (19) :9173-9200.|[2]Kathleen M. Gillooly, et al. Bruton'styrosine kinase inhibitor BMS-986142 in experimental models of rheumatoid arthritis enhances efficacy of agents representing clinical standard-of-care. PLoS One. 2017; 12 (7) : e0181782.