A potent

CEP-33779 – 500 µg

Brand:
Cayman
CAS:
1257704-57-6
Storage:
-20
UN-No:
Non-Hazardous - /

Janus kinases (JAKs) are non-receptor kinases that mediate signaling through cytokine receptors, often to members of the signal transducer and activator of transcription family.{20362} CEP-33779 is a potent, orally available inhibitor of JAK2 (IC50 = 1.3 nM).{27702} It shows 65-fold selectivity for JAK2 over JAK3.{27702} In mouse models of systemic lupus erythematosus, CEP-33779 reduces the production of inflammatory cytokines, decreases splenomegaly and lymphomegaly, and extends survival.{27702} It also diminishes inflammatory signaling and improves clinical scores in mice during collagen antibody-induced arthritis and collagen type II-induced arthritis.{27701} CEP-33779 induces regression of established colorectal tumors in mice, reducing angiogenesis and proliferation of tumor cells.{27700}  

 

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Description

A potent, orally available inhibitor of JAK2 (IC50 = 1.3 nM); reduces the production of inflammatory cytokines and blocks disease development in mouse models of lupus and arthritis; induces regression of established colorectal tumors in mice, reducing angiogenesis and proliferation of tumor cells

Formal name: N-[3-(4-methyl-1-piperazinyl)phenyl]-8-[4-(methylsulfonyl)phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-amine

Synonyms: 

Molecular weight: 462.6

CAS: 1257704-57-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|JAK Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Signaling|JAK/STAT Signaling||Research Area|Cell Biology|Cell Signaling|JAK Signaling||Research Area|Immunology & Inflammation|Autoimmunity|Lupus||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis

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