177575-17-6

AG2034 is an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 28 nM against human GARFT, and it binds with high affinity to the folate receptor (Kd of 0.0042 nM). Additionally, AG2034 is a substrate for rat liver folylpolyglutamate synthetase, with a Km of 6.4 μM. AG2034 inhibits the growth of L1210 and CCRF-CEM cells, with IC50 values of 4 nM and 2.9 nM, respectively, and it has demonstrated antitumor activity in xenograft models such as 6C3HED[1][2].

ChEBI: AG 2034 is a glutamic acid derivative.

[1] Boritzki TJ, et al. AG2034: a novel inhibitor of glycinamide ribonucleotide formyltransferase. Invest New Drugs. 1996;14(3):295-303. DOI:10.1007/BF00194533
[2] Roberts JD, et al. Phase I study of AG2034, a targeted GARFT inhibitor, administered once every 3 weeks. Cancer Chemother Pharmacol. 2000;45(5):423-7. DOI:10.1007/s002800051012
[3] Hartman PA, et al. Gradient reversed-phase high-performance liquid chromatographic separation of paldimycin (U-70,138) antibiotics and related compounds. J Chromatogr. 1987 Jan 9;385:363-8. DOI:10.1016/s0021-9673(01)94651-5