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Metabolism DHFR Pemetrexed acid

Pemetrexed acid

Catalog No. T0189   CAS 137281-23-3
Synonyms: LY231514, Pemetrexed, LY-231514 Disodium Hydrate

Pemetrexed, a guanine-derived antineoplastic agent, binds to and inhibits the enzyme thymidylate synthase (TS).

Pemetrexed acid, CAS 137281-23-3
Pack Size Availability Price/USD Quantity
10 mg In stock 32.00
25 mg In stock 40.00
50 mg In stock 57.00
100 mg In stock 74.00
200 mg In stock 103.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Pemetrexed, a guanine-derived antineoplastic agent, binds to and inhibits the enzyme thymidylate synthase (TS).
Targets&IC50 DHFR : ic50 7.2nM,   GARFT : ic50 65nM,   Thymidylate synthase : 1.3nM(Ki),  
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].
Kinase Assay AICARFT inhibition assays are carried out at room temperature by monitoring the formation of [6S]-5,6,7,8-tetrahydrofolate from 10-formyl-[6R,S]-5,6,7,8-tetrahydrofolate at A298. All solutions are purged with N2 gas prior to use. The reaction solution contains 33 mM Tris-Cl, pH 7.4, 25 mM KCl, 5 mM 2-Mercaptoethanol, 0.05 mM AICA ribonucleotide, and 16 nM (2 milliunits/mL) of AICARFT. 10-Formyl-[6R,S]-5,6,7,8-tetrahydrofolate concentrations of 0.037, 0.074, and 0.145 mM are used (0.61, 1.23, and 2.45 times its Km value, respectively). LY231514 is tested as an inhibitor at 0.08-0.8 mM (four concentrations). When the tri- and pentaglutamates of LY231514 are used as inhibitors, the concentrations are 0.0005-0.009 mM (eight concentrations). Enzyme assays are initiated by the addition of enzyme. Data is analyzed using the ENZFITTER program for competitive inhibition.
Cell Research
Pemetrexed is dissolved in DMSO and stored, and then diluted with cell culture medium before use[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×l04 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].
Animal Research
Animal Model: NOD/SCID mice
Synonyms LY231514 , Pemetrexed , LY-231514 Disodium Hydrate
Purity 98.10%
Molecular Weight 427.41
Formula C20H21N5O6
CAS No. 137281-23-3

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 100 mg/mL (233.97 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
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. 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.

Related compound libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library FDA-approved Drug Library DNA Damage & Repair Compound Library Anti-cancer Approved drug Library Anti-Metabolism Disease Compound Library Anti-cancer Metabolism Compound Library

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