Silmitasertib
Cat. No.:YN450132
产品名称: | Silmitasertib |
CAS No.: | 1009820-21-6 |
Chemical Name: | 5-[(3-chlorophenyl)amino]-benzo[c]-2,6-naphthyridine-8-carboxylic acid |
Synonyms: | CX-4945 |
分子量: | 349.77 |
分子式: | C₁₉H₁₂ClN₃O₂ |
SMILES: | O=C(C1=CC=C2C3=C(C(NC4=CC=CC(Cl)=C4)=NC2=C1)C=CN=C3)O |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | Silmitasertib (CX-4945) 是一种有效、可口服、高度选择性的CK2抑制剂,对 CK2α 和 CK2α' 的IC50值均为 1 nM。 |
IC50和靶点: | [{name:"CK2α:1 nM (IC50)'}, {"CK2α'": '1 nM (IC50)"}] |
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Pierre, F., Chua, P.C., O'Brien, 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 cancerJ. Med. Chem.54(2),635-654(2011)
Ferguson, A.D., Sheth, P.R., Basso, A.D., et al.Structural basis of CX-4945 binding to human protein kinase CK2FEBS Lett.585(1),104-110(2011)
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 efficacyCancer Res.70(24),10288-10298(2010)
Agarwal, M., Nitta, R.T., and Li, G.Casein Kinase 2: A novel player in glioblastoma therapy and cancer stem cellsJ. Mol. Genet. Med.8(1),1000094(2013)
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 cytotoxicityJ. Hematol. Oncol.6,78(2013)
Kim, H., Choi, K., Kang, H., et al.Identification of a novel function of CX-4945 as a splicing regulatorPLoS One9(4),e94978(2014)