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Technical Data
| Formula | C20H22N8O5 |
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| Molecular Weight | 454.44 | CAS No. | 59-05-2 | |
| Solubility (25°C)* | In vitro | DMSO | 91 mg/mL (200.24 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | Methotrexate, 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. Methotrexate (MTX) induces apoptosis. | ||
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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 (from reference)
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References
Customer Product Validation
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, , ChemMedChem, 2015, 10(5):804-14.
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Data from [Data independently produced by , , Oncotarget, 2016, 7(17):23439-53]
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Data from [Data independently produced by , , J Cell Physiol, 2018, 233(5):3713-3722]
Selleck's Methotrexate has been cited by 82 publications
| Identifying squalene epoxidase as a metabolic vulnerability in high-risk osteosarcoma using an artificial intelligence-derived prognostic index [ Clin Transl Med, 2024, 14(2):e1586] | PubMed: 38372422 |
| EFNB1 levels determine distinct drug response patterns guiding precision therapy for B-cell neoplasms [ iScience, 2024, 27(1):108667] | PubMed: 38155773 |
| NINJ1 regulates ferroptosis via xCT antiporter interaction and CoA modulation [ bioRxiv, 2024, 2024.02.22.581432] | PubMed: 38464226 |
| Patient- and xenograft-derived organoids recapitulate pediatric brain tumor features and patient treatments [ EMBO Mol Med, 2023, 15(12):e18199] | PubMed: 38037472 |
| USP11-mediated LSH deubiquitination inhibits ferroptosis in colorectal cancer through epigenetic activation of CYP24A1 [ Cell Death Dis, 2023, 14(7):402] | PubMed: 37414755 |
| A novel antifolate suppresses growth of FPGS-deficient cells and overcomes methotrexate resistance [ Life Sci Alliance, 2023, 6(11)e202302058] | PubMed: 37591722 |
| miR-197-3p Promotes Osteosarcoma Stemness and Chemoresistance by Inhibiting SPOPL [ J Clin Med, 2023, 12(3)1177] | PubMed: 36769824 |
| Modeling drug-induced liver injury and screening for anti-hepatofibrotic compounds using human PSC-derived organoids [ Cell Regen, 2023, 12(1):6] | PubMed: 36864321 |
| A pH-Responsive DNA Tetrahedron/Methotrexate Drug Delivery System Used for Rheumatoid Arthritis Treatment [ J Funct Biomater, 2023, 10.3390/jfb14110541] | PubMed: 37998110 |
| Multi-omics analysis based on 3D-bioprinted models innovates therapeutic target discovery of osteosarcoma [ Bioact Mater, 2022, 18:459-470] | PubMed: 35415297 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.