2704587-24-4
Chemical Structure
Fadeucravacitinib
Synonym(s): Tyk2-IN-8
- CAS No.: 2704587-24-4
- Formula:C20H19D3N8O3
- Molecular Weight:425.46
IUPAC Name: 6-(cyclopropanecarboxamido)-4-((6-(3-(1-hydroxyethyl)azetidin-1-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)amino)-N-methylpyridazine-3-carboxamide
InChIKey: BZZKEPGENYLQSC-HPRDVNIFSA-N
SMILES: [2H]C([2H])([2H])OC1=C(C2=NN(C)C=N2)C=CC=C1NC3=C(N=NC(NC(C4CC4)=O)=C3)C(NC)=O
Biological Activity: Fadeucravacitinib (Tyk2-IN-8) is an orally active selective TYK2 inhibitor with an IC50 of 5.7 nM against the JH2 pseudokinase domain. Fadeucravacitinib specifically binds to the TYK2 JH2 domain to exert allosteric inhibition, reduces JH1 kinase activity, and thereby blocks the TYK2/STAT pathway and pro-inflammatory signaling cascades. Fadeucravacitinib can be used in research related to inflammatory bowel disease[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Fadeucravacitinib | 98.04% | Fadeucravacitinib (Tyk2-IN-8) is an orally active selective TYK2 inhibitor with an IC50 of 5.7 nM against the JH2 pseudokinase domain. Fadeucravacitinib specifically binds to the TYK2 JH2 domain to exert allosteric inhibition, reduces JH1 kinase activity, and thereby blocks the TYK2/STAT pathway and pro-inflammatory signaling cascades. Fadeucravacitinib can be used in research related to inflammatory bowel disease. | ||||||||||||||||||||
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Deucravacitinib-13C,d3 | Deucravacitinib-13C,d3 is the 13C- and deuterium labeled 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. | |||||||||||||||||||||
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Deucravacitinib | 99.93% | Deucravacitinib (BMS-986165) is an orally active allosteric inhibitor of tyrosine kinase 2 (TYK2), with an IC50 of 0.2 nM and a Ki of 0.02 nM against the JH2 domain of TYK2, and it exhibits selectivity over other JAK subtypes and most of the kinome. Deucravacitinib blocks IL-23, IL-12, p-STAT1/3 and Type I IFN signaling, and inhibits Th17/Th1-mediated psoriasis inflammation. Deucravacitinib can be used in research related to moderate-to-severe plaque psoriasis, inflammatory bowel disease and systemic lupus erythematosus. | ||||||||||||||||||||
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Tyk2-IN-25 | Tyk2-IN-25 is a TYK2 inhibitor that binds to the JH2 domain of TYK2. Tyk2-IN-25 inhibits p-STAT4 and p-STAT3 in human peripheral blood mononuclear cells. Tyk2-IN-25 is applicable to research related to multiple diseases such as immune and inflammatory diseases, and neurological diseases. | |||||||||||||||||||||
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[1]. Smith J, et al. Novel compounds and methods of use. WO2021180072A1. World Intellectual Property Organization. September 16, 2021.
- [2]. Zhou Y, et al. Novel Small Molecule Tyrosine Kinase 2 Pseudokinase Ligands Block Cytokine-Induced TYK2-Mediated Signaling Pathways. Frontiers in immunology. 2022;13:884399. [Content Brief]
- [3]. Modak S, et al. B7H3-Directed Intraperitoneal Radioimmunotherapy With Radioiodinated Omburtamab for Desmoplastic Small Round Cell Tumor and Other Peritoneal Tumors: Results of a Phase I Study. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2020 Dec 20;38(36):4283-4291. [Content Brief]
