Pemetrexed

Catalog No.S5971 Batch:S597103

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
* <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.)

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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
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