A potent

CGI1746 – 10 mg

Brand:
Cayman
CAS:
910232-84-7
Storage:
-20
UN-No:
Non-Hazardous - /

CGI1746 is a potent, selective inhibitor of Bruton’s tyrosine kinase (BTK; IC50 = 1.9 nM), a non-receptor tyrosine kinase that is important in B lymphocyte development.{32058,30641} It blocks both auto-and trans-phosphorylation of BTK by occupying an SH3 binding pocket in the un-phosphorylated enzyme. CGI1746 prevents B-cell antigen receptor-mediated B lymphocyte proliferation and suppresses FCγRIII-induced TNFα, IL-1β, and IL-6 production in macrophages.{32058} It reduces cytokine levels within joints and ameliorates symptoms in a mouse model of autoantibody-induced arthritis.{32058}  

 

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Description

A potent, selective inhibitor of BTK (IC50 = 1.9 nM); prevents BCR-mediated B lymphocyte proliferation; reduces cytokine levels within joints and ameliorates symptoms in a mouse model of autoantibody-induced arthritis

Formal name: N-[3-[4,5-dihydro-4-methyl-6-[[4-(4-morpholinylcarbonyl)phenyl]amino]-5-oxo-2-pyrazinyl]-2-methylphenyl]-4-(1,1-dimethylethyl)-benzamide

Synonyms: 

Molecular weight: 579.7

CAS: 910232-84-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Non-Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling

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