Description: High affinity dihydrofolate reductase inhibitor; also inhibits thymidylate synthase, GARFT and AICART
Chemical Name:N-[4-[2-(2-Amino-4,7-dihydro-4-oxo-3H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
High affinity dihydrofolate reductase inhibitor (Ki = 7 nM). Also inhibits thymidylate synthase, AICART and glycinamide ribonucleotide formyltransferase (Ki values are 109 nM, and 3.5 μM and 9.3 μM, respectively). Indirectly activates AMPK. Inhibits proliferation of cancer cell lines in vitro.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
42.74
100
Preparing Stock Solutions
The following data is based on the product molecular weight 427.41. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.34 mL
11.7 mL
23.4 mL
5 mM
0.47 mL
2.34 mL
4.68 mL
10 mM
0.23 mL
1.17 mL
2.34 mL
50 mM
0.05 mL
0.23 mL
0.47 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Shihet al (1997) LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes. Cancer Res. 57 1116 PMID: 9067281
Rothbartet al (2010) Pemetrexed indirectly activates the metabolic kinase AMPK in human carcinomas. Cancer Res. 0 10299 PMID: 21159649