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Description: Tinostamustine (also known as EDO-S101) is a novel, potent, fisrt-in-class alkylating and pan histone-deacetylase (HDAC) inhibitor which inhibits HDAC1, HDAC2 and HDAC3 with IC50 values of 9, 9 and 25 nM, respectively and can also alkylate the DNA of cancer cells. Tinostamustine is an alkylatlng HDAC inhibitor and a fusion molecule comprising of the alkylator bendamustine and the HDAC-inhibitor vorinostat. It can potentiate the alkylating activity of the compound and/or may help to overcome resistance to other therapeutic agents. Tinostamustine was designed to allow for the exploitation of both mechanisms of action simultaneously with the goal to provide a molecule with superior efficacy over the single agents. The pharmacological testing confirms the full functional capacity of both moieties and encouraging pharmacological data raises the hope that the drug may turn out to be a great addition to the armentarium of anticancer agents.
References: Anticancer Agents Med Chem. 2016; 16(1):20-8.
Related CAS: 1793059-58-1 (HCl)
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