Pemetrexed disodium (Synonyms: LY231514 disodium)

Name: Pemetrexed disodium
Brand: MedChemExpress
SKU: HY-10820A
Rating: 5.0 (26 reviews)

Cat. No.: HY-10820A Purity: 99.95%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Pemetrexed disodium Chemical Structure

CAS No. : 150399-23-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
50 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 92	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 158	In-stock	Estimated Time of Arrival: December 31
500 mg		Get quote
1 g		Get quote

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Based on 26 publication(s) in Google Scholar

Other Forms of Pemetrexed disodium:

Pemetrexed In-stock
Pemetrexed disodium hemipenta hydrate In-stock
Pemetrexed-d₅ disodium Get quote
Pemetrexed disodium heptahydrate Get quote
Pemetrexed disodium (Standard) Get quote

24 Publications Citing Use of MCE Pemetrexed disodium

: 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.

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Protocol
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Description

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.

Clinical Trial

Molecular Weight

471.37

Formula

C₂₀H₁₉N₅Na₂O₆

CAS No.

150399-23-8

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

In Vitro:

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

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

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Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (247 KB) HNMR (271 KB) LCMS (266 KB)

Handling Instructions (2659 KB)

References

[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]

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]. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

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.

Pemetrexed disodium Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pemetrexed disodium150399-23-8LY231514 disodiumAntifolateAutophagyApoptosisInhibitorinhibitorinhibit

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Pemetrexed disodium (Synonyms: LY231514 disodium)

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24 Publications Citing Use of MCE Pemetrexed disodium

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