1. Cell Cycle/DNA Damage Autophagy Apoptosis
  2. Antifolate Autophagy Apoptosis
  3. Pemetrexed disodium

Pemetrexed disodium  (Synonyms: LY231514 disodium)

Cat. No.: HY-10820A Purity: 99.95%
COA Handling Instructions

Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.

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

Pemetrexed disodium Chemical Structure

Pemetrexed disodium Chemical Structure

CAS No. : 150399-23-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
USD 73 In-stock
Solution
10 mM * 1 mL in Water USD 73 In-stock
Solid
50 mg USD 66 In-stock
100 mg USD 92 In-stock
200 mg USD 158 In-stock
500 mg   Get quote  
1 g   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 26 publication(s) in Google Scholar

Other Forms of Pemetrexed disodium:

Top Publications Citing Use of Products

    Pemetrexed disodium purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 May 15;10(13):6048-6060.  [Abstract]

    Western blot analysis of UCHL1 levels in PEM-R cells and their parental cells. The mRNA and protein levels of UCHL1 in the PEM-R cells are significantly increased, relative to in the parental cells.

    Pemetrexed disodium purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 May 15;10(13):6048-6060.  [Abstract]

    Immunofluorescence assay showing the expression and intracellular location of UCHL1 in NSCLC cells. Increased UCHL1 levels are observed in both the cytoplasm and the nucleus of the PEM-R cells.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively[1].

    IC50 & Target

    Ki: 1.3 nM (TS), 7.2 nM (DHFR), 65 nM (GARFT)[1]

    In Vitro

    Pemetrexed (LY231514) disodium is a novel classical antifolate, the antitumor activity of which may result from simultaneous and multipie inhibition of several key folate-requiring enzymes via its polyglutamated metabolites. Pemetrexed (LY231514) is one of the best substrates that is known for the enzyme FPGS (Km=1.6 μM and Vmax/Km=621). It is likely that polyglutamation and the polyglutamated metabolites of LY231514 play profound roles in determining both the selectivity and the antitumor activity of this novel agent. Whereas LY23l5l4 only moderately inhibits TS (Ki=340 nM, recombinant mouse), the pentaglutamate of LY23l5l4 is 100-fold more potent (Ki=3.4 nM), making LY231514 one of the most potent folate-based TS inhibitors[1].

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

    In Vivo

    The group of mice treated with PC61 plus Pemetrexed demonstrates statistically longer survival than other groups. In a survival analysis, significantly better survival is observed in the group of mice treated with PC61 plus Pemetrexed compare with those treated with PC61 alone, rat IgG plus Pemetrexed, or no treatment[2].

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

    Clinical Trial
    Molecular Weight

    471.37

    Formula

    C20H19N5Na2O6

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1NC(N)=NC2=C1C(CCC3=CC=C(C=C3)C(N[C@@H](CCC(O[Na])=O)C(O[Na])=O)=O)=CN2

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    H2O : 100 mg/mL (212.15 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1215 mL 10.6074 mL 21.2148 mL
    5 mM 0.4243 mL 2.1215 mL 4.2430 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 50 mg/mL (106.07 mM); Clear solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  Saline

      Solubility: 100 mg/mL (212.15 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.95%

    References
    Cell Assay
    [1]

    Dose-response curves are generated to determine the concentration required for 50% inhibition of growth (IC50). Pemetrexed is dissolved initially in DMSO at a concentration of 4 mg/mL and further diluted with cell culture medium to the desired concentration. CCRF-CEM leukemia cells in complete medium are added to 24-well Cluster plates at a final concentration of 4.8×104 cells/well in a total volume of 2 mL. Test compounds at various concentrations are added to duplicate wells so that the final volume of DMSO is 0.5%. The plates are incubated for 72 h at 37°C in an atmosphere of 5% CO2 in air. At the end of the incubation, cell numbers are determined on a ZBI Coulter counter. Control wells usually contain 4×105 to 6×105 cells at the end of the incubation. For several studies, IC50s are determined for each compound in the presence of either 300 μM AICA, 5 μM thymidine, 100 μM hypoxanthine, or combination of 5 μM hymidine plus 100 μM hypoxanthine[1].

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

    Animal Administration
    [2]

    Mice[2]
    Female CBA mice and female NOD/SCID mice (NOD.CB17-Prkdcscid) at 6-8 wk of age are used. Premetrexed (100 mg/kg) is given i.p. from days 4-8 (5 consecutive d) to tumor-bearing mice to explore the synergistic effect when combined with anti-CD25 Ab or IgG control. The dose and schedule used for Pemetrexed in the current study is determined based on previous studies in mice.

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

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O 1 mM 2.1215 mL 10.6074 mL 21.2148 mL 53.0369 mL
    5 mM 0.4243 mL 2.1215 mL 4.2430 mL 10.6074 mL
    10 mM 0.2121 mL 1.0607 mL 2.1215 mL 5.3037 mL
    15 mM 0.1414 mL 0.7072 mL 1.4143 mL 3.5358 mL
    20 mM 0.1061 mL 0.5304 mL 1.0607 mL 2.6518 mL
    25 mM 0.0849 mL 0.4243 mL 0.8486 mL 2.1215 mL
    30 mM 0.0707 mL 0.3536 mL 0.7072 mL 1.7679 mL
    40 mM 0.0530 mL 0.2652 mL 0.5304 mL 1.3259 mL
    50 mM 0.0424 mL 0.2121 mL 0.4243 mL 1.0607 mL
    60 mM 0.0354 mL 0.1768 mL 0.3536 mL 0.8839 mL
    80 mM 0.0265 mL 0.1326 mL 0.2652 mL 0.6630 mL
    100 mM 0.0212 mL 0.1061 mL 0.2121 mL 0.5304 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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