CEP-33779 is a potent, selective, and orally bioavailable inhibitor of JAK2 with IC50 of 1.3 nM, 65-fold selective over JAK-3. CEP-33779 decreases NF-κB activation modulating the proinflammatory tumor microenvironment. CEP-33779 impacts neoplasia by restricting tumor cell proliferation and angiogenesis. CEP-33779 strongly suppresses growth of established tumors in an AOM/DSS–induced model of colorectal cancer. CEP-33779 mitigates several immune parameters associated with SLE advancement, including the protection and treatment of mice with lupus nephritis.
