Silmitasertib (CX-4945, CX4945)是有效的、可口服的、高度选择性和ATP竞争性的CK2 (casein kinase 2)抑制剂，IC₅₀值为1 nM。CX-4945在多种恶性肿瘤细胞系中皆表现出抗增殖活性。此外，CX-4945还能诱导细胞自噬并促进细胞凋亡。

参考文献

[1].Siddiqui-Jain A, et al. CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy. Cancer Res. 2010;70(24),10288-10298.

[2].Pierre F, 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. J Med Chem. 2011;54(2),635-654.

[3].Siddiqui-Jain A, et al. CK2 inhibitor CX-4945 suppresses DNA repair response triggered by DNA-targeted anticancer drugs and augments efficacy: mechanistic rationale for drug combination therapy. Mol Cancer Ther. 2012;11(4),994-1005.

[4].Bliesath J, et al. Combined inhibition of EGFR and CK2 augments the attenuation of PI3K-Akt-mTOR signaling and the killing of cancer cells. Cancer Lett. 2012;322(1),113-118.

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