5-Fluoroorotic acid

5-Fluoroorotic acid is the inhibitor for thymidylate synthase that acts as a selective agent in yeast molecular genetics. 5-Fluoroorotic acid exhibits antimalarial activity^[1][2][3]. In Vitro: 5-Fluoroorotic acid (1 mg/mL, 4-7 days) inhibits thymidylate synthase, selectively inhibits the growth of Ura+ cells with the presence of UMP synthase, and can be used for screening of Ura- mutated yeast (such as Saccharomyces cerevisiae)^[1][3].
5-Fluoroorotic acid (1 nM-100 μM, 48 h) exhibits antimalarial activity against Plasmodium falciparum with an IC₅₀ of 6.0 nM. 5-Fluoroorotic acid exhibits relatively lower cytotoxicity in mammalian cell HT-1080 with an IC₅₀ of 10 μM^[4][5].
In Vivo: 5-Fluoroorotic acid (0.2-5 mg/kg, ip, every 4 hours for 3 days) suppresses malarial parasitemia, exhibits toxicity with the absence of uridine (at a dose of 5 mg/kg) in P. yoelii-infected mouse models^[5].