CX-4945

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Description

CX-4945 (Silmitasertib) is the first orally available small molecule inhibitor of protein CK2 in clinical trials for cancer. CX-4945 (Silmitasertib) selectively binds to and inhibits the enzyme casein kinase II (CK2). Protein kinase CK2 (CK2) is involved in a variety of roles essential to the maintenance of cellular homeostasis. CK2 promotes signaling in the Akt pathway and CX-4945 suppresses the phosphorylation of Akt as well as other key downstream mediators of the pathway such as p21. CX-4945 has been reported to show broad spectrum anti-proliferative activity in multiple cancer cell lines. CX-4945 induced apoptosis and caused cell cycle arrest in cancer cells in vitro. CX-4945 exhibited a dose-dependent antitumor activity in a xenograft model of PC3 prostate cancer model and was well tolerated. In vivo time-dependent reduction in the phosphorylation of the biomarker p21 at T145 was observed by immunohistochemistry.

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