Methotrexate
Catalog No.: GC10405Purity:>98.00%
Methotrexate is an antifolate antimetabolite that effectively inhibits the activity of dihydrofolate reductase (DHFR), with an IC50 of approximately 7nM.
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Cas No.: 59-05-2
10mM (in 1mL DMSO)In Stock
$39.00
1
100mgIn Stock
$39.00
1
200mgIn Stock
$59.00
1
500mgIn Stock
$90.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $39.00 | In Stock | 1 | |
| 100mg | $39.00 | In Stock | 1 | |
| 200mg | $59.00 | In Stock | 1 | |
| 500mg | $90.00 | In Stock | 1 |
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Citations
1 publicationsPublications from researchers using this productDescription
Methotrexate is an antifolate antimetabolite that effectively inhibits the activity of dihydrofolate reductase (DHFR), with an IC50 of approximately 7nM [1]. Folic acid is essential for the biosynthesis of purine and pyrimidine bases, so methotrexate interferes with the synthesis of purines and pyrimidines required for DNA replication and cell proliferation [2]. Methotrexate also inhibits adenosine deaminase (ADA), resulting in increased extracellular adenine nucleotide levels [3]. Methotrexate has anticancer, antirheumatic, anti-inflammatory and immunomodulatory activities [4].
In vitro, methotrexate (5 μg/ml) has a wide range of IC50s against various cancer cell lines, from 6.05±0.81 nM to >1,000 nM. Methotrexate resistance in Saos-2 and MCF-7 cells The most potent, AGS and HCT-116 cells are highly sensitive to methotrexate, with IC50 of 6.05±0.81nM and 13.56±3.76nM respectively. NCI-H23 and A549 cells show similar sensitivity to methotrexate [5]. Methotrexate (3ng/ml-1μg/ml) measured the degree of drug resistance of the U-2OS cell line and found that the cell resistance was related to the increase in intracellular DHFR levels [6].
In vivo, treatment of arthritic DBA/1J mice with methotrexate (2-50 mg/kg; s.c.) dose-dependently reduced disease activity and mean paw volume and increased mean body weight percentage [7]. Methotrexate (2 mg/kg; i.p.) treats arthritis in rats and has significant anti-arthritic effects and prevents the occurrence of hematological toxicity [8].
References:
[1]Gurdag S, Khandare J, Stapels S, et al. Activity of dendrimer−methotrexate conjugates on methotrexate-sensitive and-resistant cell lines[J]. Bioconjugate chemistry, 2006, 17(2): 275-283.
[2] Rajagopalan P T R , Zhang Z , Mccourt L ,et al.Interaction of dihydrofolate reductase with methotrexate: Ensemble and single-molecule kinetics[J].Proceedings of the National Academy of Sciences, 2002, 99(21):13481-13486.
[3] Sramek M, Neradil J, Veselska R. Much more than you expected: the non-DHFR-mediated effects of methotrexate[J]. Biochimica et Biophysica Acta (BBA)-General Subjects, 2017, 1861(3): 499-503.
[4] Bedoui Y, Guillot X, Sélambarom J, et al. Methotrexate an old drug with new tricks[J]. International journal of molecular sciences, 2019, 20(20): 5023.
[5] Yoon S A , Choi J R , Kim J O ,et al. Influence of Reduced Folate Carrier and Dihydrofolate Reductase Genes on Methotrexate-Induced Cytotoxicity[J].Cancer Research & Treatment, 2010, 42(3):163-171.
[6]Serra M , Reverter B G , Maurici D ,et al.Analysis of dihydrofolate reductase and reduced folate carrier gene status in relation to methotrexate resistance in osteosarcoma cells.[J].Annals of oncology, 2004.
[7] Singh, Rakesh K.van Haandel, LeonKiptoo, et al . Methotrexate disposition, anti-folate activity and efficacy in the collagen-induced arthritis mouse model[J].European Journal of Pharmacology: An International Journal, 2019, 853.
[8] Banji D , Banji O F , Reddy K , et al. Evaluation of the concomitant use of methotrexate and curcumin on Freund's complete adjuvant-induced arthritis and hematological indices in rats[J]. Indian Journal of Pharmacology, 2011, 43(5):546-550.
Protocol
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Cell experiment [1]: |
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Cell lines |
MCF-7, AGS, A549, NCI-H23, HCT-116 and Saos-2 cell lines |
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Preparation method |
The cytotoxicity of Methotrexate was repeatedly tested at 8 different concentrations for control: 0.03, 0.1, 0.3, 1, 3, 10, 30 and 100µg/mL. The cells were incubated for 24h to allow sufficient cell adhesion, and all the microplates were incubated for a total of 72h after Methotrexate administration. |
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Reaction Conditions |
0.03, 0.1, 0.3, 1, 3, 10, 30 and 100µg/mL; 72h |
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Applications |
The IC50s of Methotrexate was in an extensively broad range from 6.05±0.81nM to>1,000nM in the cell lines. The Saos-2 and MCF-7 cells were most resistant to Methotrexate; in contrast, the AGS and HCT-116 cells were highly sensitive to Methotrexate with an IC50 of 6.05±0.81nM and 13.56±3.76nM, respectively. The NCI-H23 and A549 cells demonstrated similar sensitivity to Methotrexate. |
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Animal experiment [2]: |
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Animal models |
Male DBA/1J mice |
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Preparation method |
The Methotrexate treatment group were further stratified into 4 subgroups and administered subcutaneous Methotrexate at doses of 2, 10, 20, or 50mg/kg weekly starting on day 14 for a total of 6 doses. Disease activity scores, paw volume measurements, and animal weight were collected. |
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Dosage form |
2, 10, 20, or 50mg/kg; s.c. |
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Applications |
Methotrexate treatment resulted in a reduction in disease activity that was variable and dose-dependent. Mean paw volume measurements were significantly reduced in mice treated with Methotrexate. Mean percent body weight increased significantly in mice treated with Methotrexate. |
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References: [1] Yoon S A , Choi J R , Kim J O ,et al. Influence of Reduced Folate Carrier and Dihydrofolate Reductase Genes on Methotrexate-Induced Cytotoxicity[J].Cancer Research & Treatment, 2010, 42(3):163-171. [2] Singh, Rakesh K.van Haandel, LeonKiptoo, et al . Methotrexate disposition, anti-folate activity and efficacy in the collagen-induced arthritis mouse model[J].European Journal of Pharmacology: An International Journal, 2019, 853. |
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Product Documents
Purity:>98.00%Appearance:A solid
Biological Data
1 / 1
Chemical Properties
CAS No.
59-05-2
Chemical Name
(2S)-2-[[4-[(2,4-diaminopteridin-6-yl)methyl-methylamino]benzoyl]amino]pentanedioic acid
SMILES
CN(CC1=CN=C2C(=N1)C(=NC(=N2)N)N)C3=CC=C(C=C3)C(=O)NC(CCC(=O)O)C(=O)O
Molecular Formula
C20H22N8O5
Molecular Weight
454.44
Solubility
≥ 21.55 mg/mL in DMSO
Storage
4°C, protect from light
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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