|PemetrexedTS, DHFR,GARFT and AICARFT inhibitor|
Sample solution is provided at 25 µL, 10mM.
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|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.|
|IC50||1.3 nM (Ki)||7.2 nM (Ki)||65 nM (Ki)|
|Cas No.||150399-23-8||SDF||Download SDF|
|Synonyms||Pemetrexed disodium, Pemetrexed disodium heptahydrate, LY-231514, Pemetrexed Na|
|Solubility||>15mg/mL in DMSO||Storage||Store at -20°C|
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.
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