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Description
Methotrexate is actively transported into cells by the folate transporter. In the cell, it is converted to a high molecular weight polyglutamate metabolite by folypolyglutamate synthase that, in turn, binds to dihydrofolate reductase and inhibits its activity. Methotrexate-polyglutamate is degraded intracellularly by gamma-glutamyl hydrolase.
Methotrexate is an allosteric inhibititor of dihydrofolate reductase (DHFR), the enzyme that catalyzes the conversion of dihydrofolate to tetrahydrofolate. Since tetrahydrolfolate is required for purine and pyrimidine synthesis, methotrexate treatment results in the inhibition of DNA and RNA synthesis.
- Potent inhibitor of dihydrofolate reductase in DHFR-based protein expression systems
- Anti-cancer agent used in antitumor studies
- Effective in treatment of pyrimethamine-resistant Plasmodium vivax malaria parasites
- Shows immunosuppressive effects, e.g. in rheumatoid arthritis
Specifications
Specifications
| Melting Point | 185°C to 204°C |
| Boiling Point | 184°C to 204°C (monohydrate decomposition) |
| Quantity | 10 mg |
| Solubility Information | Soluble in alkaline solutions with decomposition.Insoluble in water, ethanol, chloroform and ether. |
| Optical Rotation | 19–24° |
| Formula Weight | 454.4 |
| Grade | USP |
| Physical Form | Powder |
Safety and Handling
- METHOTREXATE, USP Grade
- Danger
- Acute toxicity Category 3
- Reproductive toxicity Category 1A
- Skin corrosion/irritation Category 2
- Serious eye damage/eye irritation Category 2
- H301-Toxic if swallowed.
- H315-Causes skin irritation.
- H319-Causes serious eye irritation.
- H360-May damage fertility or the unborn child.
- P101-If medical advice is needed, have product container or label at hand.
- P102-Keep out of reach of children.
- P103-Read label before use.
- P280-Wear protective gloves/protective clothing/eye protection/face protection.
- P301+P310-IF SWALLOWED: Immediately call a POISON CENTER/doctor /
- P305+P351+P338-IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing.
- P321-Specific treatment (see on this label).
- P405-Store locked up.
- P501-Dispose of contents/container to .
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