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.
For research use only. We do not sell to patients.
- CAS No.: 177575-17-6
- Formula: C18H21N5O6S2
- Molecular Weight:467.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 28 nM (GARFT)[1]
Chemical Information
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CAS No. 177575-17-6
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Molecular Weight 467.52
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Formula C18H21N5O6S2
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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