Pemetrexed, Disodium Salt, Heptahydrate **

产品名称：Pemetrexed, Disodium Salt, Heptahydrate
产品货号：LC  P-7177
产品规格：1 G
Pemetrexed inhibits dihydrofolate reductase, thymidylate synthase and glycinamide ribonucleotide formyltransferase with Ki values of 7 nM, 109 nM and 9.3 µM, respectively.  Shih, C., et al.  "LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes."  Cancer Res. 57:  1116-1123 (1997).
Pemetrexed inhibits the proliferation of various human tumor cell lines, including CCRF-CEM leukemia, GC3/C1 colon carcinoma, and HCT-8 ileocecal carcinoma cells.  Thymidine demonstrated its greatest protective effect at the IC50 of pemetrexed.  However, higher drug concentrations of pemetrexed required the combination of both thymidine plus hypoxanthine to protect the tumor cells.  Shih, C., et al.  "LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes."  Cancer Res. 57:  1116-1123 (1997).
The addition of folic acid supplementation with some antifolates substantially diminished the host toxicity.  However, natural folates inhibited the activity of pemetrexed by suppressing folylpolyglutamate synthetase and thus decreasing the levels of active folylpolyglutamate pemetrexed congeners.  Zhao, R., et al.  "Marked suppression of the activity of some, but not all, antifolate compounds by augmentation of folate cofactor pools within tumor cells."  Biochem. Pharmacol. 61:  857-865 (2001).
The membrane transport system for pemetrexed includes reduced folate carrier (RFC), folate receptors, a folate transport carrier with a low-pH optimum, and RFC-independent transport at neutral pH, etc.  Chattopadhyay, S., et al.  "Pemetrexed: biochemical and cellular pharmacology, mechanisms, and clinical applications."  Mol. Cancer Ther. 6:  404-417 (2007).
Pemetrexed was approved in combination with cisplatin for the treatment of pleural mesothelioma in 2004.  Hazarika, M., et al.  "FDA drug approval summaries: pemetrexed (Alimta®)."  Oncologist 9:  482-488 (2004).
Pemetrexed was also approved for the second-line treatment of locally advanced or metastatic non-small cell lung cancer in 2004.  Cohen, M.H., et al.  "FDA drug approval summary: pemetrexed for injection (Alimta®) for the treatment of non-small cell lung cancer."  Oncologist 10:  363-368 (2005).
Pemetrexed is the active ingredient in the drug sold under the trade name Alimta®.  This drug has been approved in at least one country for use in patients with pleural mesothelioma as well as non-small cell lung cancer.  NOTE:  The pemetrexed product sold by LC Laboratories is NOT Alimta® and is NOT for human use.
Our pemetrexed product is the disodium salt heptahydrate, whose CAS number is given above. The following CAS numbers correspond to other forms of pemetrexed: 137281-23-3 for the free acid; 150399-23-8 for the anhydrous disodium salt, and 357166-30-4 for the disodium salt "hemipentahydrate" (2.5 H2O).
NOTE:  Water content may vary from lot to lot.  Please refer to the elemental analysis provided in the Certificate of Analysis to obtain the water content for each lot.
We note that one of our competitors, HouLi Biochem, as of August 16, 2011, is claiming 100% purity for their Pemetrexed, Disodium Salt, Heptahydrate.  This claim is not credible because it is physically impossible.
Storage:  Store at or below -20 ºC.  Solubility:  Very poorly soluble in DMSO; very poorly soluble in ethanol; soluble in water at 100 mg/mL; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A
 

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