| 货号 | 16246-50mg |
| 描述 | CYT387 is an ATP-competitive inhibitor of the Janus kinases JAK1 and JAK2 (IC50s = 11 and 18 nM, respectively).1,2 It displays significantly less activity against other kinases, including JAK3 (IC50 = 0.16 µM).1 At 0.5 to 1.5 µM, CYT387 causes growth suppression and apoptosis in JAK2-dependent hematopoietic cell lines.1 It is efficacious in a mouse model of JAK2V617F-dependent myeloproliferative neoplasms, although kinase domain mutations can confer resistance.1,3 CYT387 also blocks paclitaxel-induced JAK2 activation in ovarian cancer cells, preventing the development of a cancer stem cell-like population following chemotherapy.4 |
| 别名 | Momelotinib; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Tyner, J.W.,Bumm, T.G.,Deininger, J., et al. CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood 115(25), 5232-5240 (2010). 2.Furqan, M.,Mukhi, N.,Lee, B., et al. Dysregulation of JAK-STAT pathway in hematological malignancies and JAK inhibitors for clinical application. Biomark.Res. 1(1), 1-10 (2013). 3.Deshpande, A.,Reddy, M.M.,Schade, G.O.M., et al. Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms. Leukemia 26(4), 708-715 (2012). 4.Abubaker, K.,Luwor, R.B.,Zhu, H., et al. Inhibition of the JAK2/STAT3 pathway in ovarian cancer results in the loss of cancer stem cell-like characteristics and a reduced tumor burden. BMC Cancer 14, 1-22 (2014). | |
| 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 | 414.5 |
| 分子式 | C23H22N6O2 |
| CAS号 | 1056634-68-4 |
| 稳定性 | ≥ 2 years |
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