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Pemetrexed disodium (LY231514) is an antineoplastic, multitargeted antifolate which inhibits TS (thymidylate synthase), DHFR and GARFT as well as other folate dependent enzymes. By inhibiting the formation of precursor purine and pyrimidine nucleotides, pemetrexed prevents the formation of DNA and RNA, which are required for the growth and survival of both normal cells and cancer cells. Pemetrexed disodium shows the antiproliferative activity in CCRF-CEM leukemia, GC3/C1 colon carcinoma, and HCT-8 ileocecal carcinoma cells with IC50 of 25 nM, 34 nM and 220 nM, respectively. In the human H460 non-small cell lung carcinoma xenograft, Pemetrexed disodium produces a duration-dependent tumor growth delay (TGD). Pemetrexed has demonstrated antitumor activity in various tumor types as a single agent and in combination with other chemotherapeutic agents. In a phase III trial, pemetrexed (LY231514) demonstrated equivalent efficacy to docetaxel, but with significantly less toxicity, in second-line treatment of non-small-cell lung cancer.
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Source | Biochem Biophys Res Commun (2014). Figure 2. Pemetrexed disodium |
| Method | apoptosis assay | |
| Cell Lines | OS cell | |
| Concentrations | 1 μM | |
| Incubation Time | 72 h | |
| Results | Through Annexin V FACS assay, we showed that pemetrexed (1 μM) or C6 ceramide (5 μg/ml) alone only slightly induced apoptosis of U2OS cells and MG-63 cells (5–10%), combination of the two led to a significant increase of cell apoptosis. |
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Source | Biochem Biophys Res Commun (2014). Figure 1. Pemetrexed disodium |
| Method | MTT assay | |
| Cell Lines | OS cells | |
| Concentrations | 1 μM | |
| Incubation Time | 72 h | |
| Results | C6 ceramide showed most significant sensitization effect with pemetrexed at 1 μM, this concentration was chosen for further experiments. |
| Cell Experiment | |
|---|---|
| Cell lines | Human OS cell |
| Preparation method | U2OS cells were treated with pemetrexed (PMX, 1 lM) and/or C6 ceramide (C6, 5 lg/ml) for 24 h, phospho-/regular Akt and S6K1 were tested by Western blots (A). |
| Concentrations | 1 µM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | nude mice |
| Formulation | Pemetrexed disodium is dissolved in DMSO and then diluted in water. |
| Dosages | 100 mg/kg or 150 mg/kg |
| Administration | i.p. |
| Molecular Weight | 471.37 |
| Formula | C20H19N5Na2O6 |
| CAS Number | 150399-23-8 |
| Solubility (25°C) | Water 84 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Antifolate Products |
|---|
| Methotrexate
Methotrexate (Amethopterin) is an antimetabolite and antifolate agent with antineoplastic and immunosuppressant activities. |
| Folinic acid calcium salt
Folic acid is an adjuvant compound used in cancer chemotherapy. *The compound is unstable in solutions, freshly prepared is recommended |
| Sulfamethazine
Sulfamethazine is a sulfonamide antibacterial. |
| Pyrimethamine
Pyrimethamine is a dihydrofolate reductase(DHFR) inhibitor with an IC50 of 15.4 nM. |
| Methotrexate metabolite
Methotrexate metabolite is a dihydrofolate reductase potent inhibitor with an IC50 of 1 nM. |
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