| 货号 | 12094-10mg |
| 描述 | Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors.1,2 A JAK2 gene fusion mutation, JAK2V617F, that causes unchecked activation of various growth factors and cytokines, has been linked to myeloproliferative disorders.3 Lestaurtinib is a staurosporine analog that potently inhibits JAK2 kinase (IC50 = 1 nM) and downstream targets STAT5 (IC50 = 10-30 nM) and STAT3 in a human erythroleukemic cell line expressing the JAK2V617Fmutation.3,4 It has been used to reduce tumor growth in a xenograft model of pancreatic ductal adenocarcinoma, to inhibit cell growth in a trk-B overexpressing neuroblastoma xenograft model, and to block proliferation and induce apoptosis in Hodgkin lymphoma cell lines.5,6,7 Lestaurtinib has since been reported to potently inhibit the epigenetic kinase PRK1 in vitro(IC50 = 8.6 nM), inducing hypophosphorylation of histone H3 threonine 11 and blocking androgen-dependent gene expression in prostate cancer cells at a concentration of 5 μM.8 |
| 别名 | A 154475.0;CEP-701;KT 5555;SP 924; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Leonard, W.J., and OShea, J.J. JAKS AND STATS: Biological implications. Annual Reviews of Immunology 16, 293-322 (1998). 2.Yamaoka, K.,Saharinen, P.,Pesu, M., et al. The janus kinases (Jaks). Genome Biology 5(12), 1-6 (2004). 3.Verstovsek, S. Therapeutic potential of JAK2 inhibitors. Hematology Am.Soc.Hematol.Educ.Program 2009(1), 636-642 (2009). 4.Hexner, E.O.,Serdikoff, C.,Jan, M., et al. Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders. Blood 111(12), 5663-5671 (2008). 5.Miknyoczki, S.J.,Chang, H.,Klein-Szanto, A., et al. The Trk tyrosine kinase inhibitor CEP-701 (KT-5555) exhibits significant antitumor efficacy in preclinical xenograft models of human pancreatic ductal adenocarcinoma. Clinical Cancer Research 5, 2205-2212 (1999). 6.Iyer, R.,Evans, A.E.,Qi, X., et al. Lestaurtinib enhances the anti-tumor efficacy of chemotherapy in murine xenograft models of neuroblastoma. Clinical Cancer Research 16(5), 1478-1485 (2010). 7.Diaz, T.,Navarro, A.,Ferrer, G., et al. Lestaurtinib inhibition of the JAK/STAT signaling pathway in Hodgkin lymphoma inhibits proliferation and induces apoptosis. PLoS One 6(4), (2011). 8.Köhler, J.,Erlenkamp, G.,Eberlin, A., et al. Lestaurtinib inhibits histone phosphorylation and androgen-dependent gene expression in prostate cancer cells. PLoS One 7(4), (2012). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 439.5 |
| 分子式 | C25H21N3O4 |
| CAS号 | 111358-88-4 |
| 稳定性 | ≥ 2 years |
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