CX-6258
货号：
16245-1mg 基本售价：
546.0 元 规格：
1 mg
产品信息
概述| 货号 | 16245-1mg |
| 描述 | The family of Pim (Provirus Integration site for Moloney murine leukemia virus) proteins are serine/threonine kinases involved in cell survival and cell proliferation. CX-6258 is a potent, reversible inhibitor of Pim-1, -2, and -3 (IC50s = 5, 25, and 16 nM, respectively).1 It demonstrates excellent selectivity, inhibiting only FLT3 from a panel of 107 additional kinases. CX-6258 dose-dependently blocks the phosphorylation of the Pim targets Bad, 4E-BP1, and NKX3.1.1,2 It acts synergistically with the chemotherapeutics doxorubicin and paclitaxel, presumably because CX-6258 impairs Pim-mediated enhanced expression of P-glycoprotein.1 CX-6258 is orally bioavailable and inhibits the growth of MV4-11 xenografts in mice.1 |
| 别名 | Pim-Kinase Inhibitor X; |
性能| 供应商 | Cayman |
| 应用文献 |
1.Haddach, M.,Michaux, J.,Schwaebe, M.K., et al. Discovery of CX-6258. A potent, selective, and orally efficacious pan-Pim kinases inhibitor. ACS Med.Chem.Lett. 3(2), 135-139 (2011).
2.Padmanabhan, A.,Gosc, E.B. and Bieberich, C.J. Stabilization of the prostate-specific tumor suppressor NKX3.1 by the oncogenic protein kinase Pim-1 in prostate cancer cells. Journal of Cellular Biochemistry 114, 1050-1057 (2013).
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| 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 | 461.9 |
| 分子式 | C26H24ClN3O3 |
| CAS号 | 1202916-90-2 |
| 稳定性 | ≥ 2 years |
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