CEP-33779

Description: CEP33779 is a novel, potent, orally bioactive, highly selective inhibitor of JAK2 (Janus kinase) with potential antitumor and anti-inflammatory activity. It inhibits JAK2 with an IC50 of 1.8 nM, and exhibits > 40- and > 800-fold selectivity for JAK2 over JAK1 and TYK2. CEP33779 showed high activity in mice with collagen-induced arthritis (CIA) and collagen-antibody induced arthritis (CAIA). It induced regression of established colorectal tumors, reduced angiogenesis, and reduced proliferation of tumor cells. The ability of CEP-33779 to suppress growth of colorectal tumors by inhibiting the IL-6/JAK2/STAT3 signaling suggests a potential therapeutic utility of JAK2 inhibitors in multiple tumors types, particularly those with a strong inflammatory component.

References: Arthritis Res Ther. 2011 Apr 21; 13(2):R68; J Immunol. 2011 Oct 1; 187(7):3840-53; Mol Cancer Ther. 2012 Apr; 11(4):984-93.

CEP-33779; CEP 33779; CEP33779

Chemical Name: N-(3-(4-methylpiperazin-1-yl)phenyl)-8-(4-(methylsulfonyl)phenyl)-[1, 2, 4]triazolo[1, 5-a]pyridin-2-amine

InChi Key: RFZKSQIFOZZIAQ-UHFFFAOYSA-N

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)

SMILES Code: O=S(C1=CC=C(C2=CC=CN3C2=NC(NC4=CC=CC(N5CCN(C)CC5)=C4)=N3)C=C1)(C)=O