CAS: 929904-85-8

Guadecitabine sodium is a inhibitor of second-generation DNA methyltransferases (DNMT) .

Guadecitabine sodium is a pharmaceutical that inhibits the activity of DNA methyltransferases. It is used in the treatment of platinum-resistant ovarian cancer and other cancers. Guadecitabine sodium has been shown to inhibit tumor growth in mouse models of cancer. In addition, it has been shown to be more potent than decitabine at inhibiting tumor growth and metastasis. The mechanism by which guadecitabine sodium works is not fully understood, but it may involve its ability to inhibit mitochondrial membrane potential and Toll-like receptor 4 (TLR4) activation. Guadecitabine sodium has a bicyclic heterocycle structure with an ethylene bridge between two rings, which makes it structurally similar to decitabine.

Applications 2'-Deoxy-5-azacytidylyl-(3'→5')-2'-deoxy-guanosine is an DNA methylation inhibitor in vivo and was shown to effectively tolerated in tumor-free mouse and was found to be similarly effective in reducing tumor growth. References Chuang, J.C., et al.: Mole. Cancer. Therapeu., 9, 1443 (2010);