1. Cell Cycle/DNA Damage
    Antibody-drug Conjugate/ADC Related
    Apoptosis
  2. Antifolate
    DNA/RNA Synthesis
    ADC Cytotoxin
    Apoptosis
  3. Methotrexate

Methotrexate (Synonyms: Amethopterin; CL14377; WR19039)

Cat. No.: HY-14519 Purity: 99.87%
Handling Instructions

Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia).

For research use only. We do not sell to patients.

Methotrexate Chemical Structure

Methotrexate Chemical Structure

CAS No. : 59-05-2

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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
100 mg USD 60 In-stock
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Methotrexate:

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Description

Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia)[1][2][3].

IC50 & Target

Traditional Cytotoxic Agents

 

In Vivo

Methotrexate (Amethopterin) reduces thymus and spleen indices of mice. Methotrexate markedly decreases white blood cells, thymic and splenic lymphocytes at dose ≥5 mg/kg. However, there is a significant difference between the treatment plus control group and the model group (p<0.01). The combination of grape seed proanthocyanidins and Siberian ginseng eleutherosides obviously diminishes the effects of Methotrexate exposure on indices of thymus and spleens in mice[2].
Methotrexate (MTX) (2 mg/kg; i.p.; once in a week for 5 weeks) is effective in Freund's complete adjuvant-induced arthritis. The combination of Methotrexate (1 mg/kg; i.p.; once in a week for 5 weeks) and Curcumin (30 mg/kg and 100 mg/kg, thrice a week for 5 weeks; i.p.) shows a significant anti-arthritic action and protection from hematological toxicity[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

454.44

Formula

C₂₀H₂₂N₈O₅

CAS No.

59-05-2

SMILES

NC1=NC(N)=C2C(N=CC(CN(C)C3=CC=C(C(N[[email protected]@H](CCC(O)=O)C(O)=O)=O)C=C3)=N2)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (110.03 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2005 mL 11.0026 mL 22.0051 mL
5 mM 0.4401 mL 2.2005 mL 4.4010 mL
10 mM 0.2201 mL 1.1003 mL 2.2005 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

  • 3.

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

  • 4.

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice[2]
The combination of bioactive phytochemicals is administered one week prior to the Methotrexate exposure. Treatment group I: mice are given a combination of green tea polyphenols and eleutherosides from Siberian ginseng (0.2 mL/10 g, i.g. once daily) for 15 days, and a single dose of Methotrexate (2 mg/kg, i.p. once daily) is added on the 8th day. Treatment group II: mice are given a combination of grape seed proanthocyanidins and eleutherosides from Siberian ginseng for 15 days, and Methotrexate is administered on the 8th day in a similar manner. Model group: animals received distilled water instead of bioactive phytochemicals combinations for 15 days and the same Methotrexate protocol applied to this group on the 8th day. Control group: mice are given distilled water through 15 days and physiological saline instead of Methotrexate is administered on the 8th day in a similar manner. Twelve hours after the final doses, the animals are euthanized by cervical dislocation.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.87%

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Keywords:

MethotrexateAmethopterin CL14377 WR19039CL14377CL 14377CL-14377WR19039WR 19039WR-19039AntifolateDNA/RNA SynthesisADC CytotoxinApoptosisreductaseDNAsynthesisimmunosuppressantantineoplasticrheumatoidarthritislymphoblasticleukemiaInhibitorinhibitorinhibit

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Methotrexate
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