Methotrexate
Catalog No.S1210 Synonyms: NCI-C04671
Molecular Weight(MW): 454.44
Methotrexate (MTX), analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH.
3 Customer Reviews
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Toxicity of MTX (3) and toxic analogues 5 a-e on a) hY1R-expressing MDA-MB-468 and b) non-hYR-expressing HEK293 cells. Cell viability was determined by resazurin assay. Bars represent the mean±SEM of at least three independent experiments performed in triplicate. Measurements were normalized by using only HBSS, pH 7, treated cells (set at 100 %) and ethanol-treated cells (set at 0 %). Statistical significances refer to only HBSS, pH 7, treated cells indicated as a dashed line.
ChemMedChem, 2015, 10(5):804-14.. Methotrexate purchased from Selleck.
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A. Viability comparison of REH vector control, BCL6 overexpression, or BCL6 overexpression cells pre-treated with 79-6 (125μM) following exposure to three chemotherapy drugs (Ara-C [1 μM], MTX [50 μM], VCR [25 μM]). (* = p < 0.05 BCL6 OX to vector control and # = p < 0.05 BCL6 OX to BCL6 + 79-6).
Oncotarget, 2016, 7(17):23439-53. Methotrexate purchased from Selleck.
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Western blotting andrelative densitometric analyses of ERαexpression levels in regular (MCF-7) (a and a’) 4OH-tamoxifen resistant (Tam-Res) (b and b’) MCF-7cells treated for 24 hrs in complete medium with different doses of methotrexate (MTX) or vehicle (DMSO).
J Cell Physiol, 2018, 233(5):3713-3722. Methotrexate purchased from Selleck.
Purity & Quality Control
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Biological Activity
| Description | Methotrexate (MTX), analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| In vitro |
Methotrexate (0.1-10 mM) induces apoptosis of in vitro activated T cells from human peripheral blood. Methotrexate achieves clonal deletion of activated T cells in mixed lymphocyte reactions. Methotrexate can selectively delete activated peripheral blood T cells by a CD95-independent pathway. [1] Methotrexate is taken up by cells via the reduced folate carrier and then is converted within the cells to polyglutamates. Methotrexate leads to diminished production of leukotriene B4 by neutrophils stimulated ex vivo. Methotrexate polyglutamates inhibit the enzyme aminoimidazolecarboxamidoadenosineribonucleotide (AICAR) transformylase more potently than the other enzymes involved in purine biosynthesis. Methotrexate is also known to suppress TNF activity by suppressing TNF-induced nuclear factor-κB activation in vitro, in part related to a reduction in the degradation and inactivation of an inhibitor of this factor, IκBα, and probably related to the release of adenosine. Methotrexate suppresses the production of both TNF and IFN-γ by T-cell-receptor-primed T lymphocytes from both healthy human donors and RA patients. Methotrexate treatment is associated with a significant decrease of TNF-α-positive CD4+ T cells, while the number of T cells expressing the anti-inflammatory cytokine IL-10 increased. [2] |
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| In vivo | Methotrexate increases splenocyte AICAR content, raised adenosine concentrations in exudates from carrageenan-inflamed air pouches, and markedly inhibits leukocyte accumulation in inflamed air pouches in mice. Methotrexate-mediated reduction in leukocyte accumulation is partially reversed by injection of adenosine deaminase (ADA) into the air pouch, completely reverses by a specific adenosine A2 receptor antagonist, 3,7-dimethyl-1-propargylxanthine (DMPX), but not affected by an adenosine A1 receptor antagonist, 8-cyclopentyl-dipropylxanthine in mice. [3] |
Protocol
Solubility (25°C)
| In vitro | DMSO | 90 mg/mL warmed (198.04 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% DMSO+30% PEG 300+5% Tween 80+ddH2O For best results, use promptly after mixing. |
5mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 454.44 |
|---|---|
| Formula | C20H22N8O5 |
| CAS No. | 59-05-2 |
| Storage | powder |
| in solvent | |
| Synonyms | NCI-C04671 |
Bio Calculators
Molarity Calculator
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT04109300 | Not yet recruiting | Genetic: HLADQA1*05A>G screening|Other: Standard of Care | Inflammatory Bowel Diseases|Ulcerative Colitis|Crohn Disease | Western University Canada | September 1 2020 | Not Applicable |
| NCT03642795 | Not yet recruiting | Other: Questionnaire | Rheumatoid Polyarthritis | Centre Hospitalier Universitaire de Nīmes | January 2020 | -- |
| NCT03964259 | Recruiting | Drug: Intravenous fluids | Lymphoma|Acute Lymphoblastic Leukemia|Pediatric Cancer|Pediatric ALL|Pediatric Lymphoma | Virginia Commonwealth University | October 2 2019 | Phase 1 |
| NCT03960177 | Recruiting | Drug: Glucarpidase | Osteosarcoma | OHSU Knight Cancer Institute|National Cancer Institute (NCI) | March 27 2019 | Early Phase 1 |
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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