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

Pemetrexed disodium hemipenta hydrate (Synonyms: LY231514 disodium hemipenta hydrate)

Cat. No.: HY-13781 Purity: 99.78%
Handling Instructions

Pemetrexed disodium hemipenta hydrate is a novel antifolate, the Ki values of the pentaglutamate of LY231514 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 hemipenta hydrate Chemical Structure

Pemetrexed disodium hemipenta hydrate Chemical Structure

CAS No. : 357166-30-4

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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Pemetrexed disodium hemipenta hydrate:

Top Publications Citing Use of Products

    Pemetrexed disodium hemipenta hydrate 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 hemipenta hydrate 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

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Pemetrexed disodium hemipenta hydrate is a novel antifolate, the Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.

    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

    516.41

    Formula

    C₂₀H₂₄N₅Na₂O₈.₅

    CAS No.

    357166-30-4

    SMILES

    O=C(O[Na])CC[[email protected]@H](C(O[Na])=O)NC(C1=CC=C(CCC2=CNC(N=C(N)N3)=C2C3=O)C=C1)=O.[2.5H2O]

    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 : ≥ 29 mg/mL (56.16 mM)

    DMSO : 2 mg/mL (3.87 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9364 mL 9.6822 mL 19.3645 mL
    5 mM 0.3873 mL 1.9364 mL 3.8729 mL
    10 mM 0.1936 mL 0.9682 mL 1.9364 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    AICARFT inhibition assays are carried out at room temperature by monitoring the formation of [6S]-5,6,7,8-tetrahydrofolate from 10-formyl-[6R,S]-5,6,7,8-tetrahydrofolate at A298. All solutions are purged with N2 gas prior to use. The reaction solution contains 33 mM Tris-Cl, pH 7.4, 25 mM KCl, 5 mM 2-Mercaptoethanol, 0.05 mM AICA ribonucleotide, and 16 nM (2 milliunits/mL) of AICARFT. 10-Formyl-[6R,S]-5,6,7,8-tetrahydrofolate concentrations of 0.037, 0.074, and 0.145 mM are used (0.61, 1.23, and 2.45 times its Km value, respectively). LY231514 is tested as an inhibitor at 0.08-0.8 mM (four concentrations). When the tri- and pentaglutamates of LY231514 are used as inhibitors, the concentrations are 0.0005-0.009 mM (eight concentrations). Enzyme assays are initiated by the addition of enzyme. Data is analyzed using the ENZFITTER program for competitive inhibition.

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

    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
    [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×l04 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.

    References

    Purity: 99.78%

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    Keywords:

    Pemetrexed disodium hemipentaLY231514 disodium hemipentaAntifolateAutophagyApoptosisInhibitorinhibitorinhibit

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