CEP-33779

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. CEP-33779 is a potent, orally available inhibitor of JAK2 (IC50 = 1.3 nM). It shows 65-fold selectivity for JAK2 over JAK3. In mouse models of systemic lupus erythematosus, CEP-33779 reduces the production of inflammatory cytokines, decreases splenomegaly and lymphomegaly, and extends survival. It also diminishes inflammatory signaling and improves clinical scores in mice during collagen antibody-induced arthritis and collagen type II-induced arthritis. CEP-33779 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. CAS Number: 1257704-57-6. Molecular Formula: C24H26N6O2S. Formula Weight: 462.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 50 mg/ml. SMILES: CS(C1=CC=C(C2=CC=CN3C2=NC(NC4=CC=CC(N5CCN(C)CC5)=C4)=N3)C=C1)(=O)=O. InChi Code: InChI=1S/C24H26N6O2S/c1-28-13-15-29(16-14-28)20-6-3-5-19(17-20)25-24-26-23-22(7-4-12-30(23)27-24)18-8-10-21(11-9-18)33(2,31)32/h3-12,17H,13-16H2,1-2H3,(H,25,27). InChi Key: RFZKSQIFOZZIAQ-UHFFFAOYSA-N.