Pemetrexed (LY-231514) is an antifolate that inhibits thymidylate synthase (TS) (Ki = 1.3 nM) and multiple folate-requiring enzymes, such as dihydrofolate reductase (DHFR) (Ki = 7.2 nM) and glycinamide ribonucleotide formyltransferase (GARFT) (Ki = 65 nM). [1]
Pemetrexed (LY-231514) has been studied as a potential treatment option in multiple tumor types, and has been approved in 2004 for the treatment of pleural mesothelioma [2] and non-small cell lung cancer (NSCLC) [3].
A recent clinical study reveals that platinum combination with Pemetrexed (LY-231514) significantly improved the disease control rate and resulted in a tendency toward prolongation of progression-free survival in NSCLC patients who progressed after first-line epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKIs). [4]"
Technical information:
Chemical Formula: | C20H19N5Na2O6 | |
CAS #: | 150399-23-8 | |
Molecular Weight: | 471.37 | |
Purity: | > 98% | |
Appearance: | White | |
Chemical Name: | sodium (S)-2-(4-(2-(2-amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl)benzamido)pentanedioate | |
Solubility: | Up to 100 mM in DMSO | |
Synonyms: | Pemetrexed, LY-231514, LY231514 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.
Reference:
1. | Shih C, et al. LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes. Cancer Res. 1997. 57(6):1116-23. Pubmed ID: 9067281 |
2. | Hazarika M, et al. FDA drug approval summaries: pemetrexed (Alimta). Oncologist. 2004. 9(5):482-8. Pubmed ID: 15477632 |
3. | Cohen MH, et al. FDA drug approval summary: pemetrexed for injection (Alimta) for the treatment of non-small cell lung cancer. Oncologist. 2005. 10(6):363-8. Pubmed ID: 15967829 |
4. | Lee SJ, et al. Pemetrexed plus platinum versus pemetrexed alone in non-small cell lung cancer patients who have progressed after first-line EGFR TKIs. Lung Cancer. 2015. 90(2):261-6. Pubmed ID: 15477632 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.