Raltitrexed (or ZD1694) is a quinazoline-based folate analogue that selectively inhibits thymidylate synthase (TS). TS is a folate [
F0043]-dependent enzyme that catalyzes the reductive methylation of 2'-deoxyuridine-5'-monophosphate (dUMP) [
D3673] to 2'-deoxythymidine-5'-monophosphate (dTMP) [
T0845, Na salt]. This pathway is crucial for DNA synthesis, because TS is a key enzyme in the synthesis of thymidine-5’-triphosphate (dTTP) which is required exclusively for DNA synthesis. The inhibition of TS leads to DNA fragmentation and cell death. Therefore, TS represents a critical target in cancer chemotherapy. In clinical studies, raltitrexed is also used in combination with other antitumor agents. (The product is for research purpose only.)