AG2034 is an inhibitor of glycinamide ribonucleotide formyltransferase ( GARFT ), with a K i of 28 nM against human GARFT , and it binds with high affinity to the folate receptor ( K d of 0.0042 nM). Additionally, AG2034 is a substrate for rat liver folylpolyglutamate synthetase, with a K m of 6.4 µM. AG2034 inhibits the growth of L1210 and CCRF-CEM cells, with IC 50 values of 4 nM and 2.9 nM, respectively, and it has demonstrated antitumor activity in xenograft models such as 6C3HED.
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