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4-thio-2-deoxycytidine (TdCyd) is an orally bioavailable small molecule and a modified cytidine analog with potential antineoplastic activity. Upon administration, TdCyd is incorporated into DNA during replication and inhibits the activity of DNA methyltransferase 1 (DNMT1). This inhibition blocks DNA hypermethylation, leading to DNMT1 depletion and hypomethylation of DNA. As a result, tumor suppressor genes that were previously silenced by hypermethylation can be reactivated. This mechanism results in antitumor activity and inhibition of tumor cell proliferation. Preclinical studies have shown that TdCyd can inhibit tumor growth in xenograft models at well-tolerated oral doses[1][2][4][6].
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