| Bioactivity | 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]. |
| Target | IC50: 28 nM (GARFT) |
| CAS | 177575-17-6 |
| Formula | C18H21N5O6S2 |
| Molar Mass | 467.52 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Boritzki TJ, et al. AG2034: a novel inhibitor of glycinamide ribonucleotide formyltransferase. Invest New Drugs. 1996;14(3):295-303. [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. [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. |