| 货号 | 16779-500ug |
| 描述 | CX-4945 is a potent, orally bioavailable inhibitor of casein kinase 2 (CK2; Ki = 0.38 nM) that competes with ATP by filling the small ATP binding site on the catalytic CK2α subunit, conferring selectivity.1,2,3 It inhibits proliferation in a panel of cancer cell lines that overexpress CK2 and prevents tumor growth of breast and pancreatic cancer cell xenografts in mice.3 CX-4945 blocks survival and induces apoptosis in cancer stem cells and is effective against glioblastomas and acute myeloid leukemia cells.4,5 CX-4945 also inhibits Cdc2-like kinases (Clk; IC50s = 82.3, 3.8, and 90 nM for Clk1, Clk2, and Clk3, respectively), interfering with alternative splicing.6 |
| 别名 | Silmitasertib; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Pierre, F.,Chua, P.C.,OBrien, S.E., et al. Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. Journal of Medicinal Chemistry 54(2), 635-654 (2011). 2.Ferguson, A.D.,Sheth, P.R.,Basso, A.D., et al. Structural basis of CX-4945 binding to human protein kinase CK2. FEBS Letters 585(1), 104-110 (2011). 3.Siddiqui-Jain, A.,Drygin, D.,Streiner, N., et al. CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy. Cancer Research 70(24), 10288-10298 (2010). 4.Agarwal, M.,Nitta, R.T., and Li, G. Casein Kinase 2: A novel player in glioblastoma therapy and cancer stem cells. J.Mol.Genet.Med. 8(1), 1-18 (2013). 5.Quotti Tubi, L.,Gurrieri, C.,Brancalion, A., et al. Inhibition of protein kinase CK2 with the clinical-grade small ATP-competitive compound CX-4945 or by RNA interference unveils its role in acute myeloid leukemia cell survival, p53-dependent apoptosis and daunorubicin-induced cytotoxicity. J.Hematol.Oncol. 6, 1-15 (2013). 6.Kim, H.,Choi, K.,Kang, H., et al. Identification of a novel function of CX-4945 as a splicing regulator. PLoS One 9(4), e94978 (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 | 349.8 |
| 分子式 | C19H12ClN3O2 |
| CAS号 | 1009820-21-6 |
| 稳定性 | ≥ 2 years |
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