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MedKoo Cat#: 527004 | Name: AG2034

Description:

WARNING: This product is for research use only, not for human or veterinary use.

AG2034 is an inhibitor of the glycinamide ribonucleotide formyltransferase (GARFT).

Chemical Structure

AG2034
AG2034
CAS#177575-17-6

Theoretical Analysis

MedKoo Cat#: 527004

Name: AG2034

CAS#: 177575-17-6

Chemical Formula: C18H21N5O6S2

Exact Mass: 467.0933

Molecular Weight: 467.52

Elemental Analysis: C, 46.24; H, 4.53; N, 14.98; O, 20.53; S, 13.72

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
AG2034; AG-2034; AG 2034
IUPAC/Chemical Name
(2S)-2-[[5-[2-[(6S)-2-Amino-4-oxo-1,6,7,8-tetrahydropyrimido[5,4-b][1,4]thiazin-6-yl]ethyl]thiophene-2-carbonyl]amino]pentanedioic acid
InChi Key
HHKAOUMVRGSKLS-UWVGGRQHSA-N
InChi Code
InChI=1S/C18H21N5O6S2/c19-18-22-14-13(16(27)23-18)31-9(7-20-14)2-1-8-3-5-11(30-8)15(26)21-10(17(28)29)4-6-12(24)25/h3,5,9-10H,1-2,4,6-7H2,(H,21,26)(H,24,25)(H,28,29)(H4,19,20,22,23,27)/t9-,10-/m0/s1
SMILES Code
O=C(O)[C@@H](NC(C1=CC=C(CC[C@H]2CNC(NC(N)=NC3=O)=C3S2)S1)=O)CCC(O)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 467.52 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Peterson JJ. A review of synergy concepts of nonlinear blending and dose-reduction profiles. Front Biosci (Schol Ed). 2010 Jan 1;2:483-503. Review. PubMed PMID: 20036963. 2: Lee JJ, Lin HY, Liu DD, Kong M. Emax model and interaction index for assessing drug interaction in combination studies. Front Biosci (Elite Ed). 2010 Jan 1;2:582-601. PubMed PMID: 20036904; PubMed Central PMCID: PMC2974574. 3: Kong M, Lee JJ. Applying Emax model and bivariate thin plate splines to assess drug interactions. Front Biosci (Elite Ed). 2010 Jan 1;2:279-92. PubMed PMID: 20036878; PubMed Central PMCID: PMC4203317. 4: Straetemans R, Bijnens L. Application and review of the separate ray model to investigate interaction effects. Front Biosci (Elite Ed). 2010 Jan 1;2:266-78. PubMed PMID: 20036877. 5: Fang HB, Yu T, Tan M. Efficient experimental design and nonparametric modeling of drug interaction. Front Biosci (Elite Ed). 2010 Jan 1;2:258-65. PubMed PMID: 20036876. 6: Donev AN. Comparison of methods for statistical analysis of combination studies. Front Biosci (Elite Ed). 2010 Jan 1;2:250-7. PubMed PMID: 20036875. 7: Zhao L, Au JL, Wientjes MG. Comparison of methods for evaluating drug-drug interaction. Front Biosci (Elite Ed). 2010 Jan 1;2:241-9. PubMed PMID: 20036874; PubMed Central PMCID: PMC2885905. 8: Obajimi O, Keen JC, Melera PW. Inhibition of de novo purine synthesis in human prostate cells results in ATP depletion, AMPK activation and induces senescence. Prostate. 2009 Aug 1;69(11):1206-21. doi: 10.1002/pros.20971. PubMed PMID: 19434633. 9: Obajimi O, Melera PW. The depletion of cellular ATP by AG2034 mediates cell death or cytostasis in a hypoxanthine-dependent manner in human prostate cancer cells. Cancer Chemother Pharmacol. 2008 Jul;62(2):215-26. Epub 2007 Sep 25. PubMed PMID: 17896107. 10: Faessel HM, Slocum HK, Rustum YM, Greco WR. Thymidine and hypoxanthine protection patterns of the folic acid-enhanced synergies for combinations of trimetrexate plus a polyglutamylatable inhibitor of purine or thymidylate synthesis against human ileocecal HCT-8 cells. Int J Oncol. 2003 Aug;23(2):401-9. PubMed PMID: 12851689. 11: Bronder JL, Moran RG. Antifolates targeting purine synthesis allow entry of tumor cells into S phase regardless of p53 function. Cancer Res. 2002 Sep 15;62(18):5236-41. PubMed PMID: 12234990. 12: Rothem L, Ifergan I, Kaufman Y, Priest DG, Jansen G, Assaraf YG. Resistance to multiple novel antifolates is mediated via defective drug transport resulting from clustered mutations in the reduced folate carrier gene in human leukaemia cell lines. Biochem J. 2002 Nov 1;367(Pt 3):741-50. PubMed PMID: 12139489; PubMed Central PMCID: PMC1222927. 13: Bissett D, McLeod HL, Sheedy B, Collier M, Pithavala Y, Paradiso L, Pitsiladis M, Cassidy J. Phase I dose-escalation and pharmacokinetic study of a novel folate analogue AG2034. Br J Cancer. 2001 Feb 2;84(3):308-12. PubMed PMID: 11161393; PubMed Central PMCID: PMC2363746. 14: McLeod HL, Cassidy J, Powrie RH, Priest DG, Zorbas MA, Synold TW, Shibata S, Spicer D, Bissett D, Pithavala YK, Collier MA, Paradiso LJ, Roberts JD. Pharmacokinetic and pharmacodynamic evaluation of the glycinamide ribonucleotide formyltransferase inhibitor AG2034. Clin Cancer Res. 2000 Jul;6(7):2677-84. PubMed PMID: 10914709. 15: Roberts JD, Shibata S, Spicer DV, McLeod HL, Tombes MB, Kyle B, Carroll M, Sheedy B, Collier MA, Pithavala YK, Paradiso LJ, Clendeninn NJ. Phase I study of AG2034, a targeted GARFT inhibitor, administered once every 3 weeks. Cancer Chemother Pharmacol. 2000;45(5):423-7. PubMed PMID: 10803927. 16: Newell DR. Clinical pharmacokinetics of antitumor antifolates. Semin Oncol. 1999 Apr;26(2 Suppl 6):74-81. Review. PubMed PMID: 10598559. 17: Jansen G, Barr H, Kathmann I, Bunni MA, Priest DG, Noordhuis P, Peters GJ, Assaraf YG. Multiple mechanisms of resistance to polyglutamatable and lipophilic antifolates in mammalian cells: role of increased folylpolyglutamylation, expanded folate pools, and intralysosomal drug sequestration. Mol Pharmacol. 1999 Apr;55(4):761-9. PubMed PMID: 10101035. 18: Faessel HM, Slocum HK, Rustum YM, Greco WR. Folic acid-enhanced synergy for the combination of trimetrexate plus the glycinamide ribonucleotide formyltransferase inhibitor 4-[2-(2-amino-4-oxo-4,6,7,8-tetrahydro-3H-pyrimidino[5,4,6][1,4]thiazin -6-yl)-(S)-ethyl]-2,5-thienoylamino-L-glutamic acid (AG2034): comparison across sensitive and resistant human tumor cell lines. Biochem Pharmacol. 1999 Mar 1;57(5):567-77. PubMed PMID: 9952321. 19: Levasseur LM, Slocum HK, Rustum YM, Greco WR. Modeling of the time-dependency of in vitro drug cytotoxicity and resistance. Cancer Res. 1998 Dec 15;58(24):5749-61. PubMed PMID: 9865733. 20: Jansen G, Mauritz R, Drori S, Sprecher H, Kathmann I, Bunni M, Priest DG, Noordhuis P, Schornagel JH, Pinedo HM, Peters GJ, Assaraf YG. A structurally altered human reduced folate carrier with increased folic acid transport mediates a novel mechanism of antifolate resistance. J Biol Chem. 1998 Nov 13;273(46):30189-98. PubMed PMID: 9804775.