| 59-05-2 Basic information More.. |
Product Name: | Methotrexate | Synonyms: | METHOTREXATEFORINJECTION;METHOTREXATE(N-(4-(((2,4-DIAMINO-6-PTERIDINYL)METHYLAMINO)BENZOYL)-L-GLUTAMICACID);4-Amino-N10-methylfolic acid;Glutamic acid, N-[p-[[(2,4-diamino-6-pteridinyl)methyl]methylamino]benzoyl]-, L-(+)- (8CI);L-Glutamic acid, N-[4-[[(2,4-diamino-6-pteridinyl)methyl]methylamino]benzoyl]- (9CI);L-Methotrexate;Methotrexat-Ebewe;METHOTREXATEC | CAS: | 59-05-2 | MF: | C20H22N8O5 | MW: | 454.45 | EINECS: | 200-413-8 | Mol File: | 59-05-2.mol | |
Use
The drug is available in 50-, 100-, 200-, and 1,000-mg vialsfor IV use. Methotrexate is used to treat several cancer typesincluding breast cancer, bladder cancer, colorectal cancer,and head and neck cancer. The mechanism of action ofmethotrexate involves inhibition of DHFR leading to a depletionof critical reduced folates. The reduced folates arenecessary for biosynthesis of several purines and pyrimidines.Resistance to methotrexate can occur because ofdecreased carrier-mediated transport of drug into cells orincreased expression of the target enzyme DHFR. Oralbioavailability varies with dose because of saturable uptakeprocesses, and high doses are required to reach therapeuticlevels in the CNS. The majority of drug dosage is excretedunchanged in the urine. The renal excretion of methotrexateis inhibited by several carboxylic acid drugs such as penicillins,probenecid, nonsteroidal anti-inflammatory agents,and aspirin. Methotrexate enhances 5-FU antitumor effectswhen given 24 hours prior to the fluoropyrimidine.Methotrexate toxicity includes myelosuppression, mucositis,nausea, vomiting, severe headaches, renal toxicity, acutecerebral dysfunction, skin rash, and hyperpigmentation.
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59-05-2
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