Deucravacitinib

Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. Deucravacitinib inhibits IL-12/23 and type I IFN pathways. Deucravacitinib, the FDA's world first de novo deuterium, is available for study in moderate to severe plaque psoriasis[1][2].

Product Specifications

CAS Number

[1609392-27-9]

Product Name Alternative

BMS-986165

UNSPSC

12352005

Hazard Statement

H361, H372

Target

IFNAR; Interleukin Related; Isotope-Labeled Compounds; JAK

Type

Isotope-Labeled Compounds

Related Pathways

Epigenetics; Immunology/Inflammation; JAK/STAT Signaling; Others; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Purity

99.93

Solubility

DMSO : 33.33 mg/mL (ultrasonic)

Smiles

O=C(C1=NN=C(NC(C2CC2)=O)C=C1NC3=CC=CC(C4=NN(C)C=N4)=C3OC)NC([2H])([2H])[2H]

Molecular Formula

C20H19D3N8O3

Molecular Weight

425.46

Precautions

H361, H372

References & Citations

[1]Wrobleski ST, et al. Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165. J Med Chem. 2019 Jul 18.|[2]Catlett I, et al. SAT0226 A first-in-human, study of BMS-986165, a selective, potent, allosteric small molecule inhibitor of tyrosine kinase 2. Annals of the Rheumatic Diseases 2017;76:859.