Shelf life (days): 1460.0
Formulation: A solid
Formal Name: N-[4-[2-(2-amino-4,7-dihydro-4-oxo-3H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid-13C5, disodium salt, heptahydrate
Purity: ≥98%
Formula Markup: C15[13C]5H19N5O6 / 2Na [7H2O]
Formula Weight: 602.5
Notes: Pemetrexed-13C5 is intended for use as an internal standard for the quantification of pemetrexed (Item No. 14269) by GC- or LC-MS. Pemetrexed is an antifolate with anticancer activity.{22488,22487,53309} It is an inhibitor of folate-dependent enzymes involved in purine synthesis, including thymidylate synthase and dihydrofolate reductase (Kis = 109 and 7 nM, respectively, for the human recombinant enzymes), and the potency for thymidylate kinase is increased following polyglutamination of pemetrexed (Ki = 1.3 nM for pemetrexed-glu5).{22488,22487} Pemetrexed is an inhibitor of other nucleotide metabolism enzymes in a polyglutamination-dependent manner, including glycinamide ribonucleotide formyltransferase, with Ki values of 9,300 and 65 nM for the non-glutaminated and polyglutaminated mouse recombinant enzyme, respectively, and aminoimidazole carboxamide ribonucleotide formyltransferase, with Ki values of 3,600 and 265 nM for the non-glutaminated and polyglutaminated human enzyme, respectively. It inhibits proliferation of CCRF-CEM cells but not 5,10-dideazatetrahydrofolate-resistant CR15 cells (IC50s = 0.254 and 200 µM, respectively).{22488} Pemetrexed (100 mg/kg, i.p.) reduces tumor growth in A549, H1299, and PC-9 non-small cell lung cancer cell (NSCLC) mouse xenograft models but not in models using the same cell lines overexpressing thymidylate kinase.{53309}
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