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Methotrexate

Catalog No. T1485 CAS 59-05-2

Synonyms: NCI-C04671, WR19039, Amethopterin, CL14377

Methotrexate (WR19039) is a folate analog, an inhibitor of the dihydrofolate reductase DHFR. Methotrexate has antimetabolic, antitumor, and immunosuppressive activities, and is commonly used in rheumatoid arthritis and various tumors.

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Methotrexate, CAS 59-05-2

Pack Size	Availability	Price/USD
50 mg	In stock	$ 38.00
100 mg	In stock	$ 54.00
200 mg	In stock	$ 81.00
500 mg	In stock	$ 142.00
1 mL * 10 mM (in DMSO)	In stock	$ 54.00

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Purity: 99.46%

Purity: 96.84%

Biological Description

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Description	Methotrexate (WR19039) is a folate analog, an inhibitor of the dihydrofolate reductase DHFR. Methotrexate has antimetabolic, antitumor, and immunosuppressive activities, and is commonly used in rheumatoid arthritis and various tumors.
Targets&IC50	DHFR (human):24 nM
In vitro	METHODS: Six pediatric leukemia and lymphoma cell lines, NALM-6, NALM-16, JURKAT, CEM, RAMOS, and NAMALWA, were treated with Methotrexate (0.002-5 μM) for 120 h, and the proliferation inhibitory activity of the cells was assayed using the SRB method. RESULTS: The median IC50 of Methotrexate against tumor cells was 78 nM, and the IC50 of the six tumor cells ranged from 33-133 nM. [1] METHODS: Human ovarian cancer cells SKOV-3 were treated with Methotrexate (15-50 μM) for 24 h. Apoptosis was detected using AO/EtBr probe. RESULTS: Methotrexate induced apoptosis in SKOV-3 cells. [2]
In vivo	METHODS: To test for chronic toxicity, Methotrexate (0.25-6 mg/kg) was administered intraperitoneally to C57BL/6, DBA/2, and C3H mice five times per week for 12-18 months. RESULTS: The 0.25-2 mg/kg dose was well tolerated with minimal cytostasis in lymphoid tissues, testis and skin. 3-6 mg/kg dose produced well-known acute to subacute hematopoietic and gastrointestinal injuries leading to early death. [3] METHODS: To examine the mode of action in different types of rheumatoid arthritis (RA) and multiple sclerosis (MS) models, Methotrexate (0.1-5 mg/kg) was injected intraperitoneally once a day for fourteen days into RA and MS models with different pathogenesis. RESULTS: Methotrexate showed strong ameliorative effects in classical RA models such as CIA and PIA as well as in MS and EAE models.Methotrexate acts only prior to and dependent on T-cell activation in T-cell activated diseases. [4]
Cell Research	Methotrexate (MTX) is dissolved in DMSO and stored, and then diluted with appropriate media before use[1]. Each cell line is studied in growth inhibition experiments using 96-well microtiter plates. As antifols are schedule dependent, preliminary experiments are aimed at defining the longest duration of exposure that would allow for continuous logarithmic phase growth of cells without changing of the culture media while maintaining a linear relationship between SRB optical density and cell number. Twenty-four hours after cell plating, the cell lines are exposed to the antifol for 120 h (three replicates per experiment). To ensure that a complete sigmoidal survival-concentration curve could be observed, the following drug concentrations are studied: Methotrexate (0.002-5 μM), AMT (0.0001-1 μM), PXD (0.0003-10 μM), TLX (0.0002-0.5 μM). Experiments are repeated at least twice[1].

Synonyms	NCI-C04671, WR19039, Amethopterin, CL14377
Molecular Weight	454.44
Formula	C20H22N8O5
CAS No.	59-05-2

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 83 mg/mL (182.6 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Norris RE, et al. Clinical potency of methotrexate, aminopterin, talotrexin and pemetrexed in childhood leukemias. Cancer Chemother Pharmacol. 2010 May;65(6):1125-30. 2. AlBasher G, et al. Methotrexate-induced apoptosis in human ovarian adenocarcinoma SKOV-3 cells via ROS-mediated bax/bcl-2-cyt-c release cascading. Onco Targets Ther. 2018 Dec 17;12:21-30. 3. Freeman-Narrod M, et al. Chronic toxicity of methotrexate in mice. J Natl Cancer Inst. 1977 Mar;58(3):735-41. 4. Lange F, et al. Methotrexate ameliorates T cell dependent autoimmune arthritis and encephalomyelitis but not antibody induced or fibroblast induced arthritis. Ann Rheum Dis. 2005 Apr;64(4):599-605.

Citations

1. Li X, Xi B, Miao Y, et al. Nintedanib ameliorates imiquimod-induced psoriasis in mice by inhibiting NF-κB and VEGFR2 signaling. International Immunopharmacology. 2021, 100: 108129. 2. Zhao Y, Li Y, Zhu R, et al.RPS15 interacted with IGF2BP1 to promote esophageal squamous cell carcinoma development via recognizing m6A modification.Signal Transduction and Targeted Therapy.2023, 8(1): 224. 3. Kutbi D, Almalki R S.Valsartan Mitigates the Progression of Methotrexate-Induced Acute Kidney Injury in Rats via the Attenuation of Renal Inflammation and Oxidative Stress.Journal of Inflammation Research.2024: 2233-2243.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library EMA Approved Drug Library Drug-induced Liver Injury (DILI) Compound Library Pediatric Drug Library Approved Drug Library Glutamine Metabolism Compound Library

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Keywords

Methotrexate 59-05-2 Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair Metabolism Dehydrogenase DNA/RNA Synthesis Antifolate NCI-C 04671 WR-19039 antineoplastic WR 19039 ADC Cytotoxin arthritis rheumatoid synthesis ADC Payload Inhibitor lymphoblastic reductase leukemia immunosuppressant NCI-C04671 NCI-C-04671 CL-14377 WR19039 Amethopterin inhibit CL14377 DNA CL 14377 inhibitor

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