[CAS NO. 150399-23-8]  Pemetrexed disodium

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PRODUCTS SPECIFICATIONS [150399-23-8]

Catalog
HY-10820A
Brand
MCE
CAS
150399-23-8

DESCRIPTION [150399-23-8]

Overview

MDLMFCD07779402
Molecular Weight471.37
Molecular FormulaC20H19N5Na2O6
SMILESO=C1NC(N)=NC2=C1C(CCC3=CC=C(C=C3)C(N[C@@H](CCC(O[Na])=O)C(O[Na])=O)=O)=CN2

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


Summary

Pemetrexed disodium (LY231514 disodium) is an antifolate , the K i s 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 [1] .


IC50 & Target

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


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] .

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] .

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


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT00109096 Eli Lilly and Company
Ovarian Neoplasms|Primary Peritoneal Cancer
June 2005 Phase 2
NCT04512430 Fundación GECP
Non Small Cell Lung Cancer|EGFR Gene Mutation
December 2, 2020 Phase 2
NCT01783197 Canadian Cancer Trials Group|AstraZeneca
Non Small Cell Lung Cancer
January 30, 2013 Phase 1

Appearance

Solid


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:

H 2 O : ≥ 100 mg/mL ( 212.15 mM )

* "≥" means soluble, but saturation unknown.

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
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: Saline

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

  • 2.

    Add each solvent one by one: PBS

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

* All of the co-solvents are available by MCE.


Synonyms

L-Glutamic acid, N-[4-[2-(2-amino-4,7-dihydro-4-oxo-3H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-, sodium salt (1:2)
L-Glutamic acid, N-[4-[2-(2-amino-4,7-dihydro-4-oxo-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-, disodium salt
1H-Pyrrolo[2,3-d]pyrimidine, L-glutamic acid deriv.
Tifolar
Pemetrexed disodium
Rolazar
LY 231514
Alimta
LY 231514 disodium
Pemetrexed sodium