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MV16 is a novel hybrid homo-aza (lactam) steroidal antimetabolite currently under preclinical investigation for the treatment of gastrointestinal malignancies, specifically pancreatic and colorectal cancers. It belongs to a class of steroidal conjugates designed to enhance the selectivity and toxicokinetics of traditional antimetabolites such as 5-fluorouracil and methotrexate. MV16 functions as a dual inhibitor of thymidylate synthase (TS) and dihydrofolate reductase (DHFR), enzymes that are critical for DNA synthesis and cellular proliferation. By targeting these pathways, the compound induces cell cycle arrest and promotes apoptosis in cancer cells. While part of a series of synthesized compounds (including CS23 and KA44), MV16 represents a specific structural approach to overcoming resistance in difficult-to-treat gastrointestinal tumors.
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