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: 137281-23-3

Selleck's Pemetrexed has been cited by 26 publications

Purity & Quality Control

Batch: Purity: 99.59%
99.59

Related compound libraries

Choose Selective Thymidylate Synthase Inhibitors

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
NCT06010277 Recruiting NSCLC|Mesothelioma|Thymoma Amphia Hospital|Albert Schweitzer Hospital February 6 2023 Phase 4

Chemical lnformation & 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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Pemetrexed | Pemetrexed supplier | purchase Pemetrexed | Pemetrexed cost | Pemetrexed manufacturer | order Pemetrexed | Pemetrexed distributor