Genz-644282

Genz-644282 is a non-camptothecin small molecule inhibitor of topoisomerase I with potential antineoplastic activity. By binding to and inhibiting the enzyme topoisomerase I (TOP1), it prevents the repair of single-strand DNA breaks and disrupts DNA replication in tumor cells. This leads to cytotoxicity through double-strand break formation and inhibition of tumor cell growth. Genz‑644282 has demonstrated potent activity against a wide range of human tumor cell lines—including those resistant to camptothecin—with IC50 values ranging from low nanomolar to micromolar concentrations. It was developed for intravenous administration in oncology indications but clinical development was discontinued after phase 1 trials for solid tumors[1][4][5][7][8].

Other names

2,3-dimethoxy-12-(2-(methylamino)ethyl)-[1,3]dioxolo[4',5':4,5]benzo[1,2-h]benzo[c][1,6]naphthyridin-13(12H)-one8,9-dimethoxy-5-(2-N-methylaminoethyl)-2,3-methylenedioxy-5H-dibenzo(c,h)(1,6)naphthyridin-6-one529488-28-6