Denopterin

Denopterin is a dihydrofolate reductase (DHFR) inhibitor and an antifolate agent. Denopterin is an antimetabolite that has toxic effects on cells and can be used for cancer^[1]. IC50 & Target:Dihydrofolate reductase (DHFR); Antifolate^[1] In Vitro: Antibody-drug conjugates (ADCs) have great promise as anti-cancer drugs. In recent years, there has been increasing applications of the pyrrolobenzo-diazepine dimer (PBD) class of cytotoxic payloads as ADC therapeutics due to PBDs’extream potency against most of the US National Cancer Institute’s (NCI’s) NCI 60-tumor-cell line panels along with unique mechanism of antitumor antibiotics activity. All PBDs are usually conjugated to an antibody with one conditionally stable linker, because it is normally believed that linkers of ADCs must be stable while the ADC is circulating in the blood to limit off-target toxicity, but allow for release of the drug once it is inside the target cancer cells^[1].