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Deucravacitinib CAS# 1609392-27-9

Deucravacitinib (BMS-986165) is a selective, oral allosteric inhibitor of tyrosine kinase 2 (TYK2). Unlike JAK1/2/3 inhibitors, it binds the regulatory pseudokinase (JH2) domain of TYK2 with high affinity (IC50 ~1 nM), preventing activation without blocking the ATP-binding catalytic site. In preclinical studies, deucravacitinib potently inhibited IL-12, IL-23, and type I interferon signaling pathways in human immune cells, reducing STAT phosphorylation and downstream cytokine production (IC50 values in the low nanomolar range). In murine models of psoriasis and autoimmune inflammation, it significantly reduced disease severity. Pharmacokinetic studies confirmed good oral exposure, supporting its advancement into clinical trials for immune-mediated diseases.
📌 参考资料/链接:
Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165By: Wrobleski, Stephen T. ; et alJournal of Medicinal Chemistry (2019), 62(20), 8973-8995

📄 详细内容

CAS No. 1609392-27-9 Deucravacitinib synthetic routes


Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165By: Wrobleski, Stephen T. ; et alJournal of Medicinal Chemistry (2019), 62(20), 8973-8995
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