Home Apoptosis Thymidylate Synthase inhibitor - DHFR inhibitor - DNA/RNA Synthesis inhibitor - Autophagy activator - Apoptosis related activator Pemetrexed For research use only.

Pemetrexed

Synonyms: LY231514

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.

Pemetrexed Chemical Structure

Pemetrexed Chemical Structure

CAS No. 137281-23-3

Purity & Quality Control

Pemetrexed Related Products

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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models Female severe combined immunodeficient (SCID)-Beige mice injected with PC-9 cells
Dosages 100 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06378892 Recruiting
Non Small Cell Lung Cancer Metastatic|ALK Gene Mutation
Centro di Riferimento Oncologico - Aviano
 March 15 2024 Phase 2
NCT06010277 Recruiting
NSCLC|Mesothelioma|Thymoma
Amphia Hospital|Albert Schweitzer Hospital
 February 6 2023 Phase 4

Chemical Information & Solubility

Molecular Weight 427.41 Formula

C20H21N5O6
CAS No. 137281-23-3 SDF --
Smiles NC1=NC(=O)C2=C([NH]C=C2CCC3=CC=C(C=C3)C(=O)NC(CCC(O)=O)C(O)=O)N1
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 85 mg/mL ( (198.87 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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