TLK58747

TLK58747 is a small molecule DNA-alkylating prodrug developed by Telik, Inc. It is characterized as a next-generation alkylating agent designed for broad antitumor activity and an improved safety profile compared to traditional alkylators. Preclinical studies have demonstrated that TLK58747 inhibits the growth of various human cancer cell lines, including those for breast, lung, colorectal, ovarian, pancreatic, and prostate cancers, as well as glioma and leukemia, with IC50 values ranging from 2 to 78 μM. As a prodrug, it likely undergoes activation to release an active alkylating moiety that covalently binds to DNA, leading to cell cycle arrest and apoptosis in malignant cells.