• Methotrexate

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SKU: M027

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Methotrexate is a selective agent for DHFR transfected cells and an anticancer compound that inhibits the metabolism of folic acid.

TOKU-E offers three forms of methotrexate: methotrexate (M027), methotrexate sodium (M031), and methotrexate, Evopure® (M091). In aqueous solution, methotrexate sodium is freely soluble. Methotrexate is practically insoluble in water.

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    Mechanism of Action

    In cancerous cells, methotrexate acts as an allosteric inhibitor of dihydrofolate reductase (DHFR), an enzyme involved in the folic acid metabolic pathway. Folic acid is essential in cells because it is required for thymidine and purine synthesis. Methotrexate therefore acts as a nucleic acid synthesis inhibitor.


    Cancer Applications

    Methotrexate sodium salt acts as a chemotherapeutic agent by inhibiting nucleic acid synthesis in cancer cells.

    Eukaryotic Cell Culture Applications

    Methotrexate is commonly used in the dihydrofolate reductase (DHFR) selection system as a selection antibiotic to select for dihydrofolate reductase (DHFR) deficient CHO cells (Chinese hamster ovary) that have been transfected with DHFR genes. Methotrexate inhibits the activity of DHFR; however, cells that overproduce DHFR can tolerate higher concentrations of methotrexate. In most cases, overproducing DHFR cells produce more recombinant protein than lower DHFR producing cells.



    Immunosuppressive Medications. (2017). Retrieved from The Johns Hopkins Lupus Center, https://www.hopkinslupus.org/lupus-treatment/lupus-medications/immunosuppressive-medications/

    Fairbanks, L. D., and Et Al. "Methotrexate Inhibits the First Committed Step of Purine Biosynthesis in Mitogen-stimulated Human T-lymphocytes: A Metabolic Basis for Efficacy in Rheumatoid Arthritis?" Biochemistry Journal 342.1 (1999): 143-52. www.ncbi.gov. Web. 6 Sept. 2012.

    Kingston, RE. "Amplification Using CHO Cell Expression Vectors." Current Protocols in Molecular Biology. U.S. National Library of Medicine, Nov. 2002. Web. 23 Dec. 2016.

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