177575-17-6
Chemical Structure
AG2034
- CAS No.: 177575-17-6
- Formula:C18H21N5O6S2
- Molecular Weight:467.52
IUPAC Name: (5-(2-((S)-2-amino-4-oxo-4,6,7,8-tetrahydro-1H-pyrimido[5,4-b][1,4]thiazin-6-yl)ethyl)thiophene-2-carbonyl)-L-glutamic acid
InChIKey: HHKAOUMVRGSKLS-UWVGGRQHSA-N
SMILES: O=C1C2=C(NC(N)=N1)NC[C@@H](S2)CCC3=CC=C(C(N[C@H](C(O)=O)CCC(O)=O)=O)S3
Biological Activity: 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].
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AG2034 | 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. | |||||||||||||||||||||
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- [1]. Boritzki TJ, et al. AG2034: a novel inhibitor of glycinamide ribonucleotide formyltransferase. Invest New Drugs. 1996;14(3):295-303. [Content Brief]
- [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. [Content Brief]
Keywords
