Decernotinib - CAS 944842-54-0
Catalog number:
944842-54-0
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
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Targets:
JAK
Description:
Decernotinib, also known as VX-509 or VRT-831509 or adelatinib, is an oral, selective Janus kinase 3 (JAK3) inhibitor being developed by Vertex. VX-509 may represent a new approach to treating an underlying disease mechanism that triggers inflammation in a number of debilitating diseases, including RA. In immune-mediated diseases, JAK3 is an essential component of the immune signaling cascade. This cascade ultimately contributes to abnormal immune response that results in chronic inflammation and, in the case of RA, irreversible damage to cartilage and bones. Based on in vitro data, VX-509 has demonstrated a high level of selectivity for inhibition of JAK3 compared to JAK1- and JAK2-dependent assays, and this high level of selectivity was confirmed in clinical studies where dose-related inhibition of a JAK3-dependent biomarker was observed while little to no effect was shown against a JAK2/JAK1-dependent biomarker.
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Appearance:
Solid powder
Synonyms:
Decernotinib; adelatinib; MZK2GP0RHK; SureCN2630387; CHEMBL3039513; VX-509; VX509; VX 509; VRT-831509; VRT831509;
MSDS:
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Current Developer:
Vertex.
1.VX-509 (Decernotinib), an Oral Selective JAK-3 Inhibitor, in Combination With Methotrexate in Patients With Rheumatoid Arthritis.
Genovese MC1, van Vollenhoven RF2, Pacheco-Tena C3, Zhang Y4, Kinnman N4. Arthritis Rheumatol. 2016 Jan;68(1):46-55. doi: 10.1002/art.39473.
OBJECTIVE: To assess the efficacy and safety of decernotinib (VX-509), an oral selective inhibitor of JAK-3, in patients with rheumatoid arthritis (RA) in whom the response to methotrexate treatment was inadequate.
2.Efficacy of VX-509 (decernotinib) in combination with a disease-modifying antirheumatic drug in patients with rheumatoid arthritis: clinical and MRI findings.
Genovese MC1, Yang F2, Østergaard M3, Kinnman N2. Ann Rheum Dis. 2016 Apr 15. pii: annrheumdis-2015-208901. doi: 10.1136/annrheumdis-2015-208901. [Epub ahead of print]
OBJECTIVE: To assess early effects on joint structures of VX-509 in combination with stable disease-modifying antirheumatic drug (DMARD) therapy using MRI in adults with rheumatoid arthritis (RA).
3.VX-509 (decernotinib) is a potent and selective janus kinase 3 inhibitor that attenuates inflammation in animal models of autoimmune disease.
Mahajan S1, Hogan JK1, Shlyakhter D1, Oh L1, Salituro FG1, Farmer L1, Hoock TC2. J Pharmacol Exp Ther. 2015 May;353(2):405-14. doi: 10.1124/jpet.114.221176. Epub 2015 Mar 11.
Cytokines, growth factors, and other chemical messengers rely on a class of intracellular nonreceptor tyrosine kinases known as Janus kinases (JAKs) to rapidly transduce intracellular signals. A number of these cytokines are critical for lymphocyte development and mediating immune responses. JAK3 is of particular interest due to its importance in immune function and its expression, which is largely confined to lymphocytes, thus limiting the potential impact of JAK3 inhibition on nonimmune physiology. The aim of this study was to evaluate the potency and selectivity of the investigational JAK3 inhibitor VX-509 (decernotinib) [(R)-2-((2-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-yl)amino)-2-methyl-N-(2,2,2-trifluoroethyl)butanamide] against JAK3 kinase activity and inhibition of JAK3-mediated signaling in vitro and JAK3-dependent physiologic processes in vivo. These results demonstrate that VX-509 potently inhibits JAK3 in enzyme assays (Ki = 2.
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CAS 944842-54-0 Decernotinib

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