Art. -Nr.: HY-10820A

Pemetrexed disodium

(Synonyms: LY231514 disodium)

40 Cited Publications

Kundenbewertung

Based on 40 publication(s) in Google Scholar

Pemetrexed disodium (LY231514 disodium) is an antifolate, the K_is of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.

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Reinheit: 99.79%
CAS. Nr.: 150399-23-8
Formel: C₂₀H₁₉N₅Na₂O₆
Molecular Weight:471.37

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Pemetrexed disodium Chemical Structure

CAS. Nr.: 150399-23-8

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One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (40)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Ki: 1.3 nM (TS), 7.2 nM (DHFR), 65 nM (GARFT)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	3.29 μM Compound: 3; PTX	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 30927565]
GES1	CC₅₀	22.62 μM Compound: 3; PTX	Cytotoxicity against human GES-1 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against human GES-1 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 30927565]
HepG2	IC₅₀	3.73 μM Compound: 3; PTX	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 30927565]
L02	CC₅₀	30.69 μM Compound: 3; PTX	Cytotoxicity against human L02 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 30927565]
OVCAR-3	IC₅₀	4.35 μM Compound: 3; PTX	Antiproliferative activity against human OVCAR3 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human OVCAR3 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 30927565]
SGC-7901	IC₅₀	6.96 μM Compound: 3; PTX	Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 30927565]

In Vitro

Pemetrexed (LY231514) disodium is a novel classical antifolate, the antitumor activity of which may result from simultaneous and multipie inhibition of several key folate-requiring enzymes via its polyglutamated metabolites. Pemetrexed (LY231514) is one of the best substrates that is known for the enzyme FPGS (K_m=1.6 μM and V_max/K_m=621). It is likely that polyglutamation and the polyglutamated metabolites of LY231514 play profound roles in determining both the selectivity and the antitumor activity of this novel agent. Whereas LY23l5l4 only moderately inhibits TS (K_i=340 nM, recombinant mouse), the pentaglutamate of LY23l5l4 is 100-fold more potent (K_i=3.4 nM), making LY231514 one of the most potent folate-based TS inhibitors^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The group of mice treated with PC61 plus Pemetrexed demonstrates statistically longer survival than other groups. In a survival analysis, significantly better survival is observed in the group of mice treated with PC61 plus Pemetrexed compare with those treated with PC61 alone, rat IgG plus Pemetrexed, or no treatment^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 150399-23-8
Appearance Solid
Molecular Weight 471.37
Formel C₂₀H₁₉N₅Na₂O₆
Color White to off-white
SMILES

O=C1NC(N)=NC2=C1C(CCC3=CC=C(C=C3)C(N[C@@H](CCC(O[Na])=O)C(O[Na])=O)=O)=CN2
Synonyms

LY231514 disodium
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (40)

All Cell Proliferation/Viability AssayApoptosis AnalysisCell Imaging/StainingFlow CytometryWBIF

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Journal Impact Factor

Mol Cancer

Organoids derived from patients provide a new opportunity for research and individualized treatment of malignant peritoneal mesothelioma. [Abstract]

2024 Jan 10;23(1):12. PMID: 38200517
Mol Cell

Metabolic Diversity in Human Non-Small Cell Lung Cancer Cells. [Abstract]

2019 Dec 5;76(5):838-851.e5. PMID: 31564558

Pemetrexed disodium purchased from MedChemExpress. Usage Cited in: Mol Cell. 2019 Dec 5;76(5):838-851.e5. [Abstract]

The relationship between SerG6m3 and Pemetrexed disodium (0.01-1.0 μM; 3 d) IC₅₀.
Adv Sci (Weinh)

Deep Learning-Powered Scalable Cancer Organ Chip for Cancer Precision Medicine. [Abstract]

2026 Feb 3:e16660. PMID: 41632021
J Clin Invest

Serine hydroxymethyltransferase 2 expression promotes tumorigenesis in rhabdomyosarcoma with 12q13-q14 amplification. [Abstract]

2021 Aug 2;131(15):e138022. PMID: 34166228
Theranostics

The deubiquitinating enzyme UCHL1 promotes resistance to pemetrexed in non-small cell lung cancer by upregulating thymidylate synthase. [Abstract]

2020 May 15;10(13):6048-6060. PMID: 32483437

Pemetrexed disodium purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 May 15;10(13):6048-6060. [Abstract]

Western blot analysis of UCHL1 levels in PEM-R cells and their parental cells. The mRNA and protein levels of UCHL1 in the PEM-R cells are significantly increased, relative to in the parental cells.

Pemetrexed disodium purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 May 15;10(13):6048-6060. [Abstract]

Immunofluorescence assay showing the expression and intracellular location of UCHL1 in NSCLC cells. Increased UCHL1 levels are observed in both the cytoplasm and the nucleus of the PEM-R cells.
J Exp Clin Cancer Res

FL496, an FL118-derived small molecule, induces growth inhibition, senescence, and apoptosis of malignant pleural mesothelioma (MPM) cells, and exhibits anti-MPM tumor efficacy strikingly superior to the pemetrexed-cisplatin combination. [Abstract]

2025 Oct 21;44(1):293. PMID: 41121175
J Control Release

Effective combination of liposome-targeted chemotherapy and PD-L1 blockade of murine colon cancer. [Abstract]

2023 Jan:353:490-506. PMID: 36460179

Pemetrexed disodium purchased from MedChemExpress. Usage Cited in: J Control Release. 2023 Jan:353:490-506. [Abstract]

Cell viability of MC38 and CT26 cells after incubation with DTX, PMX, DTX+PMX, DTX-LPs,PMX-LPs, and DTX/PMX-LPs for 48 and 72 hours (n = 4, equivalent PMX (Pemetrexed) concentration is 0.048, 0.16, 1.2, 6, 30 µg/ml).

Pemetrexed disodium purchased from MedChemExpress. Usage Cited in: J Control Release. 2023 Jan:353:490-506. [Abstract]

The apoptotic rate after treatment with different Pemetrexed (1.37 μg/mL; 24 h) of drugs and formulations
Cell Rep Med

Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]

2023 Feb 21;4(2):100911. PMID: 36657446
Pharmacol Res

Time-dependent proteomics and drug response in expanding cancer cells. [Abstract]

2024 May 9:204:107208. PMID: 38729587
J Pharm Anal

Increasing the tumour targeting of antitumour drugs through anlotinib-mediated modulation of the extracellular matrix and the RhoA/ROCK signalling pathway. [Abstract]

2024 Aug;14(8):100984. PMID: 39258171
Dev Cell

A pathological role of O-GlcNAcylation-driven TR11B production and function in lung adenocarcinoma. [Abstract]

2025 Sep 3:S1534-5807(25)00530-1. PMID: 40930100
Acta Pharmacol Sin

Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]

2021 Jan;42(1):108-114. PMID: 32398685
ACS Appl Mater Interfaces

Feedback-Amplified Drug Delivery of αPD-L1-Modified Lipoplatin for Chronological Synergy in NSCLC through PD-L1 Upregulation. [Abstract]

2025 Oct 8;17(40):55861-55875. PMID: 40997865
Cell Death Discov

Targeting mitochondrial one-carbon enzyme MTHFD2 together with pemetrexed confers therapeutic advantages in lung adenocarcinoma. [Abstract]

2022 Jul 5;8(1):307. PMID: 35790743

Pemetrexed disodium purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2022 Jul 5;8(1):307. [Abstract]

The IC50 value of pemetrexed ( 0.039 to 50 μM, 5 days) in A549 cells.

Pemetrexed disodium purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2022 Jul 5;8(1):307. [Abstract]

A549 and H1299 cells were treated with pemetrexed (5 μM), DS18561882 (10 μM), or combination for 5 days. Cell proliferative abilities were detected by MTT assay.
Br J Cancer

SETDB1 tumour suppressor roles in near-haploid mesothelioma involve TP53. [Abstract]

2023 Aug;129(3):531-540. PMID: 37369845
Int J Pharm X

Bio-inspired self-assembly of omega-3 fatty acids and peptides for responsive drug delivery. [Abstract]

2026 May 5:11:100558. PMID: 42205116
Commun Biol

Serine hydroxymethyltransferase as a potential target of antibacterial agents acting synergistically with one-carbon metabolism-related inhibitors. [Abstract]

2022 Jun 23;5(1):619. PMID: 35739195
Eur J Pharmacol

GART promotes multiple myeloma malignancy via tumor stemness mediated by activating the HSP90α/CDK6/β-catenin axis. [Abstract]

2025 Apr 2:996:177584. PMID: 40185325
Int Immunopharmacol

Pemetrexed ameliorates Con A-induced hepatic injury by restricting M1 macrophage activation. [Abstract]

2023 Nov 3;125(Pt A):111158. PMID: 37925950
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
Adv Ther

2024 Jul 18.
Sci Rep

Functional personalized complex combination nano therapy for osteosarcoma. [Abstract]

2025 Oct 16;15(1):36227. PMID: 41102354
Bioengineering (Basel)

Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]

2025 Oct 19;12(10):1121. PMID: 41155119
Heliyon

Synergistic effects of MK-1775 and gemcitabine on cytotoxicity in non-small cell lung cancer. [Abstract]

2024 Nov 8;10(22):e40299. PMID: 39605823
Eur J Med Res

Long non-coding RNA NORAD serves as a promoter of oncogenesis and inhibits ferroptosis via miR-144-3p-mTOR-ferritinophagy axis in cancer. [Abstract]

2025 Aug 4;30(1):704. PMID: 40760677
Hum Cell

Hyaluronic acid-modified milk exosomes carrying ZNF516 inhibit ABCC5 and contribute to pemetrexed sensitivity in lung adenocarcinoma. [Abstract]

2025 Apr 19;38(3):92. PMID: 40253507
Integr Cancer Ther

Chinese Herbal Compound Xiaoliu Pingyi Recipe Inhibits the Growth of Lung Adenocarcinoma by Regulating the Tumor Vascular Microenvironment. [Abstract]

2024 Jan-Dec:23:15347354241273962. PMID: 39223822
Clin Transl Oncol

Establishment of an acquired lorlatinib-resistant cell line of non-small cell lung cancer and its mediated resistance mechanism. [Abstract]

2022 Nov;24(11):2231-2240. PMID: 35852680
Odontology

Accumulated cytotoxicity of CDK inhibitor dinaciclib with first-line chemotherapy drugs in salivary adenoid cystic carcinoma cells. [Abstract]

2020 Apr;108(2):300-311. PMID: 31529315

Pemetrexed disodium purchased from MedChemExpress. Usage Cited in: Odontology. 2020 Apr;108(2):300-311. [Abstract]

Cell proliferation and viability of ACC-2 cell lines treated with Pemetrexed disodium (0.01-2 μg/mL; 48 h) were measured by the Cell Counting Kit-8 (CCK-8).

Pemetrexed disodium purchased from MedChemExpress. Usage Cited in: Odontology. 2020 Apr;108(2):300-311. [Abstract]

Pemetrexed disodium (0.5 μg/mL; 48 h) caused significant cytotoxicity effects on ACC-2 cells.

Pemetrexed disodium purchased from MedChemExpress. Usage Cited in: Odontology. 2020 Apr;108(2):300-311. [Abstract]

Pemetrexed disodium (0.5 μg/mL; 12 h) increased early stage apoptotic and total apoptotic cells in ACC-2 cells.

Pemetrexed disodium purchased from MedChemExpress. Usage Cited in: Odontology. 2020 Apr;108(2):300-311. [Abstract]

Pemetrexed disodium (0.5 μg/mL; 24 h) decreased RNAP II levels in ACC-2 cells.
Pharmacol Res Perspect

Applicability of free drug hypothesis to drugs with good membrane permeability that are not efflux transporter substrates: A microdialysis study in rats. [Abstract]

2020 Apr;8(2):e00575. PMID: 32266794
Beilstein J Org Chem

Structural diversity in the host-guest complexes of the antifolate pemetrexed with native cyclodextrins: gas phase, solution and solid state studies. [Abstract]

2017 Oct 25:13:2252-2263. PMID: 29114329
Biol Methods Protoc

Optimizing drug sensitivity assays in patient-derived tumor organoids: a comparison of IC50 estimation methods and experimental parameters. [Abstract]

2025 Feb 13;10(1):bpaf012. PMID: 40060949
Res Sq

2025 Sep 7.
bioRxiv

2025 August 15.
bioRxiv

2025 January 22.
bioRxiv

2025 January 21.
bioRxiv

2024 June 12.
Research Square Print

September 27th, 2022.
University of Texas

2015.

Lösungsmittel & Löslichkeit

In Vitro:

H₂O : 100 mg/mL (212.15 mM; ultrasonic and warming and heat to 60°C)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1215 mL

10.6074 mL

21.2148 mL

5 mM

0.4243 mL

2.1215 mL

4.2430 mL

10 mM

0.2121 mL

1.0607 mL

2.1215 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS

Solubility: 50 mg/mL (106.07 mM); Clear solution; Need ultrasonic

Protocol 2

Add each solvent one by one: Saline

Solubility: 100 mg/mL (212.15 mM); Clear solution; Need ultrasonic

Protokoll

Cell Assay^[1]

Dose-response curves are generated to determine the concentration required for 50% inhibition of growth (IC₅₀). Pemetrexed 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 at a final concentration of 4.8×10⁴ cells/well in a total volume of 2 mL. Test compounds at various concentrations are added to duplicate wells so that the final volume of DMSO is 0.5%. The plates are incubated for 72 h 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. Control wells usually contain 4×10⁵ to 6×10⁵ cells at the end of the incubation. 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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]

Mice^[2]
Female CBA mice and female NOD/SCID mice (NOD.CB17-Prkdc^scid) at 6-8 wk of age are used. Premetrexed (100 mg/kg) is given i.p. from days 4-8 (5 consecutive d) to tumor-bearing mice to explore the synergistic effect when combined with anti-CD25 Ab or IgG control. The dose and schedule used for Pemetrexed in the current study is determined based on previous studies in mice.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Shih C, et al. LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes. Cancer Res. 1997 Mar 15;57(6):1116-23. [Content Brief]

[2]. Anraku M, et al. Synergistic antitumor effects of regulatory T cell blockade combined with pemetrexed in murine malignantmesothelioma. J Immunol. 2010 Jul 15;185(2):956-66. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O	1 mM	2.1215 mL	10.6074 mL	21.2148 mL	53.0369 mL
	5 mM	0.4243 mL	2.1215 mL	4.2430 mL	10.6074 mL
	10 mM	0.2121 mL	1.0607 mL	2.1215 mL	5.3037 mL
	15 mM	0.1414 mL	0.7072 mL	1.4143 mL	3.5358 mL
	20 mM	0.1061 mL	0.5304 mL	1.0607 mL	2.6518 mL
	25 mM	0.0849 mL	0.4243 mL	0.8486 mL	2.1215 mL
	30 mM	0.0707 mL	0.3536 mL	0.7072 mL	1.7679 mL
	40 mM	0.0530 mL	0.2652 mL	0.5304 mL	1.3259 mL
	50 mM	0.0424 mL	0.2121 mL	0.4243 mL	1.0607 mL
	60 mM	0.0354 mL	0.1768 mL	0.3536 mL	0.8839 mL
	80 mM	0.0265 mL	0.1326 mL	0.2652 mL	0.6630 mL
	100 mM	0.0212 mL	0.1061 mL	0.2121 mL	0.5304 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Pemetrexed disodium

40 Cited Publications

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Pemetrexed disodium

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Publications Citing Use of MedChemExpress (MCE) Pemetrexed disodium

Biologische Aktivität

Chemical Information

Publications (40)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Pemetrexed disodium Related Classifications

HY-10820A Related Classifications