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

Pemetrexed disodium (Synonyms: LY231514 disodium)

Cat. No.: HY-10820A Purity: 99.99%
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
10 mM * 1 mL in Water USD 66 In-stock
Estimated Time of Arrival: December 31
50 mg USD 60 In-stock
Estimated Time of Arrival: December 31
100 mg USD 84 In-stock
Estimated Time of Arrival: December 31
200 mg USD 144 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Pemetrexed disodium:

Top Publications Citing Use of Products

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

    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 MCE. Usage Cited in: Theranostics. 2020 May 15;10(13):6048-6060.

    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

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    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].

    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].

    Clinical Trial
    Molecular Weight

    471.37

    Formula

    C₂₀H₁₉N₅Na₂O₆

    CAS No.

    150399-23-8

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    H2O : ≥ 100 mg/mL (212.15 mM)

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.2121 mL 1.0607 mL 2.1215 mL
    *Please refer to the solubility information to select the appropriate solvent.
    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

    Purity: 99.99%

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    Keywords:

    Pemetrexed disodiumLY231514 disodiumAntifolateAutophagyApoptosisInhibitorinhibitorinhibit

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