Pemetrexed

Catalog No.S5971 Batch:S597102

Technical Data

Formula

C₂₀H₂₁N₅O₆

Molecular Weight

427.41

CAS No.

137281-23-3

Solubility (25°C)*

In vitro

DMSO

85 mg/mL (198.87 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution

5%DMSO 1 Corn oil

10.0mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Pemetrexed (LY231514) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.

Targets

Thymidylate synthase ^[1] (Cell-free assay)	DHFR ^[1] (Cell-free assay)	GARFT ^[1] (Cell-free assay)
1.3 nM(Ki)	7.2 nM(Ki)	65 nM(Ki)

In vitro

Osimertinib+pemetrexed treatment delays the emergence of resistance relative to monotherapy in vitro, also down-regulates the expression of the anti-apoptotic gene PLK1 in PC-9 and H1975.^[4]

In vivo

The combination of omepetinib and pemetrexed enhances apoptosis via a PLK1 signaling pathway, and the anti-tumor effect against xenografts harboring the EGFR mutation in vivo.^[4]

Protocol (from reference)

Cell Assay:^{^[4]}	Cell lines PC-9 and NCI-H1975 (H1975) cells Concentrations 0.001, 0.01, 0.1, 1, 10 μM Incubation Time 72 h Method Cells are plated in 96-well tissue culture plates at 5,000 cells/well and incubated at 37 ℃ for 24 h. Cells are then incubated with titrated concentrations of the drugs (0.001, 0.01, 0.1, 1, 10 μM) or vehicle (DMSO) at 37 ℃ for 72 h. Cell numbers are estimated using the Counting Kit-8. Protein extraction and western blotting are performed. Apoptosis assays are performed using the Annexin V-FITC Apoptosis Detection Kit.
Animal Study:^{^[4]}	Animal Models Female severe combined immunodeficient (SCID)-Beige mice injected with PC-9 cells Dosages 100 mg/kg Administration i.p.

Cell Assay:^{^[4]}

Cell lines
PC-9 and NCI-H1975 (H1975) cells
Concentrations
0.001, 0.01, 0.1, 1, 10 μM
Incubation Time
72 h
Method
Cells are plated in 96-well tissue culture plates at 5,000 cells/well and incubated at 37 ℃ for 24 h. Cells are then incubated with titrated concentrations of the drugs (0.001, 0.01, 0.1, 1, 10 μM) or vehicle (DMSO) at 37 ℃ for 72 h. Cell numbers are estimated using the Counting Kit-8. Protein extraction and western blotting are performed. Apoptosis assays are performed using the Annexin V-FITC Apoptosis Detection Kit.

Animal Study:^{^[4]}

Animal Models
Female severe combined immunodeficient (SCID)-Beige mice injected with PC-9 cells
Dosages
100 mg/kg
Administration
i.p.

References

[4] Takano N, et al. Anticancer Res. 2022 Feb;42(2):709-722.

+ Expand

Selleck's Pemetrexed has been cited by 33 publications

AMG 193, a Clinical Stage MTA-Cooperative PRMT5 Inhibitor, Drives Antitumor Activity Preclinically and in Patients With MTAP-Deleted Cancers [ Cancer Discov, 2024, 10.1158/2159-8290.CD-24-0887]	PubMed: 39282709
Neoadjuvant sintilimab plus chemotherapy in EGFR-mutant NSCLC: Phase 2 trial interim results (NEOTIDE/CTONG2104) [ Cell Rep Med, 2024, 5(7):101615]	PubMed: 38897205
Metabolic Hallmarks for Purine Nucleotide Biosynthesis in Small Cell Lung Carcinoma [ Mol Cancer Res, 2024, 22(1):82-93]	PubMed: 37773022
A novel lncRNA-hidden polypeptide regulates malignant phenotypes and pemetrexed sensitivity in A549 pulmonary adenocarcinoma cells [ Amino Acids, 2024, 56(1):15]	PubMed: 38351332
Protocol for generation of and high-throughput drug testing with patient-derived colorectal cancer organoids [ STAR Protoc, 2024, 5(2):103090]	PubMed: 38809757
Crosstalk with lung fibroblasts shapes the growth and therapeutic response of mesothelioma cells [ Cell Death Dis, 2023, 10.1038/s41419-023-06240-x]	PubMed: 37938546
Exploring the Molecular Players behind the Potentiation of Chemotherapy Effects by Durvalumab in Lung Adenocarcinoma Cell Lines [ Pharmaceutics, 2023, 15(5)1485]	PubMed: 37242727
Exploring the Molecular Players behind the Potentiation of Chemotherapy Effects by Durvalumab in Lung Adenocarcinoma Cell Lines [ Pharmaceutics, 2023, 15(5)1485]	PubMed: 37242727
Exploring the Molecular Players behind the Potentiation of Chemotherapy Effects by Durvalumab in Lung Adenocarcinoma Cell Lines [ Pharmaceutics, 2023, 15(5)1485]	PubMed: 37242727
Gastrodin destabilizes survivin and overcomes pemetrexed resistance [ Cell Signal, 2023, 110:110851]	PubMed: 37586466

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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