Pemetrexed Disodium Hydrate

Catalog No.S7785 Synonyms: LY-231514 Disodium Hydrate

Pemetrexed Disodium Hydrate Chemical Structure

Molecular Weight(MW): 516.42

Pemetrexed Disodium Hydrate is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively.

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Cited by 6 Publications

3 Customer Reviews

  • Role of PARP and BER in the synergy between PTX and GMX in A549 cells. Cells were pretreated ±1 umol/L olaparib (2 hours) then sequentially ±150 nmol/L PTX (24 hours), then ± GMX 12 nmol/L (48 hours). PAR modification of proteins and γ-H2AX levels were measured in extracts treated as in A by Western blotting.

    Cancer Res 2014 74(21), 5948-54. Pemetrexed Disodium Hydrate purchased from Selleck.

    Cell viability of U2OS cells after indicated pemetrexed in different concentrations or plus C6 ceramide (C6, 5 ug/ml) treatment was tested by MTT assay.

    Biochem Biophys Res Commun 2014 452(1), 72-8. Pemetrexed Disodium Hydrate purchased from Selleck.

  • A549 cells were treated with pemetrexed and/or MK1775 for 72 hours and counted by flow cytometry and the number of live cells relative to untreated is depicted.

    Mol Cancer Ther 2013 12, 2675-84. Pemetrexed Disodium Hydrate purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description Pemetrexed Disodium Hydrate is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively.
Targets
TS [1] DHFR [1] GARFT [1]
()
1.3 nM(Ki) 7.2 nM(Ki) 65 nM(Ki)
In vitro

Pemetrexed disodium shows the antiproliferative activity in CCRF-CEM leukemia, GC3/C1 colon carcinoma, and HCT-8 ileocecal carcinoma cells with IC50 of 25 nM, 34 nM and 220 nM, respectively. [1] A recent study shows that cisplatin plus Pemetrexed combined with SOCS-1 gene delivery shows the antitumor effect by inhibition of cell proliferation, invasiveness, and induction of apoptosis in MPM cells infected with adenovirus-expressing SOCS-1 vector. [2]

In vivo In the human H460 non-small cell lung carcinoma xenograft, Pemetrexed disodium produces a duration-dependent tumor growth delay (TGD). [3]

Protocol

Kinase Assay:[1]
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Enzyme Assays and Methods. :

TS activity is assayed using a spectrophotometric method, which involved monitoring the increase in absorbance at 340 nm resulting from formation of the product, 7,8-dihydrofolate. The assay buffer contains 50 mM N-tris[hydroxymethyljmethyl-2-aminoethanesulfonic acid, 25 mM MgC12, 6.5 mM formaldehyde, 1 mM EDTA, and 75 mM 2-mercaptoethanol, pH 7.4. The concentrations of deoxyuridylate monophosphate, 6R-MTHF, and hIS are 100 μM, 30μM and 30 nM (1.7 milliunits/mL), respectively. At the 6R-MTHF concentration, an uninhibited reaction and six concentrations of inhibitor are assayed. Ki app values are determined by fitting the data to the Morrison equation using nonlinear regression analysis with the aid of the program ENZFITTER. Ki values are calculated using the equation: Ki app= Ki(1 + [S]/Km), where [S] is equal to 30 μM and Km is equal to 3 μM. DHFR activity is assayed spectrophotometrically by monitoring the dis appearance of the substrates NADPH and 7,8-dihydrofolate at 340 nm. The reaction takes place at 25°C in 0.5 mL of 50 mM potassium phosphate buffer, which contains 150 mM KC1 and 10 nM 2-mercaptoethanol, pH 7.5, and 14 nM (0.34 milliunitlmL) DHFR. The NADPH concentration is 10 μM and 7,8-dihydrofolate is varied at 5, 10, or 15 μM. At each 7,8-dihydrofolate concentration, an uninhibited reaction and seven concentrations of inhibitor are assayed. The ENZFITI'ER microcomputer program is used to obtain Ki app values by fitting the data to the Morrison equation by nonlinear regression analysis. Ki app= Ki(1 + [S]/Km), where [S] is equal to the concentration of 7,8-dihydrofolate used and Km of 7,8-dihydrofolate is equal to 0.15 μM. GARFT activity is assayed spectrophotometrically by monitoring the increase of absorbance resulting from formation of the product 5,8-dideazafolate at 295 nm. The reaction solvent contains 75 mM HEPES, 20% glycerol, and 50 mM a-thioglygerol, pH 7.5, at 25°C. The concentrations of substrates and enzyme used are 10 μM α,β-glycinamide ribonucleotide, 0-10 μM 10-formyl-5,8-dideazafolic acid, and 10 nM (1.9 milliunits/mL) GARFT. Ki values are calculated using the Enzyme Mechanism program of the Beckman DU640 spectrophotometer, which uses nonlinear regression analysis to fit data to the Michaelis-Menten equation for competitive inhibition.
Cell Research:[1]
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  • Cell lines: CCRF-CEM leukemia, GC3/C1 colon carcinoma, and HCT-8 ileocecal carcinoma cells.
  • Concentrations: 0-30 μM
  • Incubation Time: 72 hours
  • Method: Dose-response curves are generated to determine the concentration required for 50% inhibition of growth (IC50). Pemetrexed disodium 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 in a total volume of 2.0 mL. Pemetrexed disodium at various concentrations are added to duplicate wells so that the final volume of DMSO is 0.5%. The plates are incubated for 72 hour 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. 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. For adherent tumor cells, a modification of the original MTT colorimetric assay is used to measure cell cytotoxicity. The human tumor cells are seeded in 100 μL assay medium/well in 96-well flat-bottomed tissue culture plates. The assay medium contains folic acid-free RPMI 1640 supplemented with 10% FCS and either 2 nM folinic acid or 2.3 μM folic acid as the sole folate source. Well 1A is left blank. Stock solutions of antifolates are prepared in Dulbecco's PBS at 1 mg/mL, and a series of 2-fold dilutions are subsequently made in PBS. Ten-μL aliquots of each concentration are added to triplicate wells. Plates are incubated for 72 hours at 37 °C in a humidified atmosphere of 5% CO2-in-air. MTT is dissolved in PBS at 5 mg/mL, 10 μL of stock MTF solution are added to each well of an assay, and the plates are incubated at 37 °C for 2 additional hours. Following incubation, 100 μL of DMSO are added to each well. After thorough formazan solubilization, the plates are read on a Dynatech MR600 reader, using a test wavelength of 570 nm and a reference wavelength of 630 nm. The IC50 is determined as the concentration of drug required to inhibit cell growth by 50% compared to an untreated controls.
    (Only for Reference)
Animal Research:[3]
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  • Animal Models: EMT-6 mammary carcinoma, the human HCT 116 colon carcinoma, and the human H460 non-small cell lung carcinoma are injected s.c. into the nude mice.
  • Formulation: Pemetrexed disodium is dissolved in DMSO and then diluted in water.
  • Dosages: 100 mg/kg or 150 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro Water 100 mg/mL warmed (193.64 mM)
DMSO Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 516.42
Formula

C20H21N5O6.5/2H2O.2Na

CAS No. 357166-30-4
Storage powder
in solvent
Synonyms LY-231514 Disodium Hydrate

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03298763 Recruiting Genetic: MSCTRAIL|Drug: Placebo Adenocarcinoma of Lung University College London March 5 2019 Phase 1|Phase 2
NCT03656549 Recruiting Drug: Pemetrexed Non Small Cell Lung Cancer|Mesothelioma Radboud University|ZonMw: The Netherlands Organisation for Health Research and Development February 1 2019 Phase 2
NCT03655821 Recruiting Drug: Pemetrexed Non Small Cell Lung Cancer|Mesothelioma Radboud University|ZonMw: The Netherlands Organisation for Health Research and Development February 1 2019 Phase 4
NCT03526900 Recruiting Drug: Atezolizumab Non-small Cell Lung Cancer Stage IV Spanish Lung Cancer Group July 7 2018 Phase 2

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DHFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID