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PemetrexedTS, DHFR,GARFT and AICARFT inhibitor

Pemetrexed

Catalog No. A4390
Size Price Stock Qty
Evaluation Sample $28.00 In stock
10mg $84.00 In stock
50mg $331.00 In stock
200mg $1,037.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Pemetrexed

Related Biological Data

Pemetrexed

Related Biological Data

Pemetrexed

Biological Activity

Description Pemetrexed is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively.
Targets TS DHFR GARFT      
IC50 1.3 nM (Ki) 7.2 nM (Ki) 65 nM (Ki)      

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Chemical Properties

Cas No. 150399-23-8 SDF Download SDF
Synonyms Pemetrexed disodium, Pemetrexed disodium heptahydrate, LY-231514, Pemetrexed Na
Chemical Name disodium;(2S)-2-[[4-[2-(2-amino-4-oxo-1,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]amino]pentanedioate
Canonical SMILES C1=CC(=CC=C1CCC2=CNC3=C2C(=O)N=C(N3)N)C(=O)NC(CCC(=O)[O-])C(=O)[O-].[Na+].[Na+]
Formula C20H19N5Na2O6 M.Wt 471.37
Solubility Limited solubility Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Pemetrexed (also known as pemetrexed disodium) is a novel antifolate antimetabolite targeting multiple enzymes involved in both pyrimidine and purine synthesis. Pemetrexed is an analog of the classic antifolate GARFYT inhibitor lometroxol with a similar chemical structure, where the pyrazine ring in the pterine portion of folic acid and the benzylic nitrogen in the bridge portion of folic acid are replaced by a pyrrole ring and a methylene group respectively. Pemetrexed potently inhibits TS, DHFR, and GARFT as well as AICARFT but with a lesser potency and exhibits autitumor activity in a broad range of tumors, including non-small cell lung carcinoma, malignant mesothelioma, and carcinomas of the breast, colorectum, uterine cervix, head and neck, and bladder.

Reference

Luis Paz-Ares, Susana Bezares, Jose M. Tabernero, Daniel Castellanos, and Hernan Cortes-Funes. Review of a promising new agent-pemetrexed disodium. Cancer 2003; 97(8 Suppl):2056-2063