| 货号 | 16732-500ug |
| 描述 | 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.1 CEP-33779 is a potent, orally available inhibitor of JAK2 (IC50 = 1.3 nM).2 It shows 65-fold selectivity for JAK2 over JAK3.2 In mouse models of systemic lupus erythematosus, CEP-33779 reduces the production of inflammatory cytokines, decreases splenomegaly and lymphomegaly, and extends survival.2 It also diminishes inflammatory signaling and improves clinical scores in mice during collagen antibody-induced arthritis and collagen type II-induced arthritis.3 CEP-33779 induces regression of established colorectal tumors in mice, reducing angiogenesis and proliferation of tumor cells.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Yamaoka, K.,Saharinen, P.,Pesu, M., et al. The janus kinases (Jaks). Genome Biology 5(12), 1-6 (2004). 2.Lu, L.D.,Stump, K.L.,Wallace, N.H., et al. Depletion of autoreactive plasma cells and treatment of lupus nephritis in mice using CEP-33779, a novel, orally active, selective inhibitor of JAK2. Journal of Immunology 187(7), 3840-3853 (2011). 3.Stump, K.L.,Lu, L.D.,Dobrzanski, P., et al. A highly selective, orally active inhibitor of Janus kinase 2, CEP-33779, ablates disease in two mouse models of rheumatoid arthritis. Arthritis Research & Therapy 13(2), 1-15 (2011). 4.Seavey, M.M.,Lu, L.D.,Stump, K.L., et al. Therapeutic efficacy of CEP-33779, a novel selective JAK2 inhibitor, in a mouse model of colitis-induced colorectal cancer. Molecular Cancer Therapeutics 11(4), 984-993 (2012). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 462.6 |
| 分子式 | C24H26N6O2S |
| CAS号 | 1257704-57-6 |
| 稳定性 | ≥ 2 years |
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