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AG2034

CAT: 0804-HY-10819Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-10819Size:1 Each
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Description
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].
CAS Number
177575-17-6
UNSPSC
12352005
Target
Antifolate
Type
Reference compound
Related Pathways
Cell Cycle/DNA Damage
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/ag2034.html
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
Molecular Formula
C18H21N5O6S2
Molecular Weight
467.52
References & Citations
[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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Phase 1

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CatalogName
T26572-01AG2034

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