Raltitrexed
Thymidylate synthase inhibitor / Raltitrexed is an inhibitor of thymidylate synthase with significantly increased potency in many cancer cell lines when compared with 5-fluorouracil.1,2 It is also an inhibitor of the methyltransferase G9a (IC50 = 120 nM) and decreased Aß aggregates in C. elegans indicating therapeutic potential for the treatment of Alzheimer’s disease.3
Biochemicals & reagents
112887-68-0
ICI D 1694; ZD1694
1) Marsham et al. (1991) Quinazoline Antifolate Thymidylate Synthase Inhibitors: Heterocyclic Benzoyl Ring Modifications; J. Med. Chem. 34 1594 2) Jackman et al. (1995) ZD1694(Tomudex): A New Thymidylate Synthase Inhibitor with Activity in Colorectal Cancer; Eur. J. Cancer 31A 1277 3) Jana et al. (2023) Repurposing of Raltitrexed as an Effective G91/EHMT2 Inhibitor and Promising Anti-Alzheimer's Agent; ACS Med. Chem. Lett. 14 1531
-20°C
TARGET: DNA; Protein methyltransferase -- PATHWAY: DNA damage -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Cancer; Neurodegeneration