Trimetrexate glucuronate Struktur

Trimetrexate glucuronate

Bezeichnung:Trimetrexate glucuronate

CAS-Nr82952-64-5

Englisch Name:Trimetrexate glucuronate

CBNumberCB6850867

SummenformelC25H33N5O10

Molgewicht563.56

MOL-Datei82952-64-5.mol

Trimetrexate glucuronate physikalisch-chemischer Eigenschaften

storage temp.	Store at -20°C
Aggregatzustand	Solid
Farbe	Off-white to light yellow

Gefahreninformationscode (GHS)

Trimetrexate glucuronate Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Trimetrexate glucuronate is a nonclassical antifolate introduced in the U.S.A. and Canada as second-line therapy for the treatment of Pneumocystis carinii pneumonia (PCP) and toxoplasmosis in AIDS patients who are refractory or intolerant to co-trimoxazole therapy. Trimetrexate glucuronate is reportedly to be in clinical trials for the treatment of several types of cancer including colorectal, gastric, pancreas, prostate, bladder, lung, breast, head, and neck cancers. It is also in early clinical trials for topical use in treating psoriasis and as an oral drug to treat rheumatoid arthritis. The mechanism of action of trimetrexate glucuronate is via inhibition of the enzyme dihydrofolate reductase which mediates the reduction of dihydrofolate to tetrahydrofolic acid and results in disruption of DNA, RNA and protein synthesis, with consequent cell death. Due to its toxicity to bone marrow and the GI tract, trimetrexate glucuronate must be concurrently administered with leucovorin as a rescue agent.
Originator
Warner-Lambert (U.S.A.)
Verwenden
CI 898 Glucuronate is a dihydrofolate reductase (DHFR) inhibitor.
Verwenden
Antineoplastic.
Manufacturing Process
A mixture of 2,4-diamino-5-methyl-6-[(3,4,5- trimethoxyanilino)methyl]quinazoline (1.0 g) and glucuronic acid (0.7 g) in methanol (65 ml) is heated to dissolve the solid. The solution is cooled to 10°C and filtered to remove a small amount of solid. The filtrate is heated to reflux and ethyl acetate is added to the cloud point. The warm solution is filtered then slowly cooled. The solid that forms is collected, washed first with ethylacetate, then with ether and dried in vacuo at 60°C to give the 4- diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl]quinazoline D_x0002_glucuronate as a yellow powder with no definite melting point.
Trademarks
Neutrexin (MedImmune).
Therapeutic Function
Antineoplastic
Biologische Aktivität
Potent lipophilic inhibitor of dihydrofolate reductase (DHFR) that displays antineoplastic and antiprotozoal properties. Inhibits protozoal, bacterial and human DHFR with IC 50 values of 1.4, 6.1 and 3.2 nM respectively. Affects G 1 /S phase cell cycle progression.

Trimetrexate glucuronate Upstream-Materialien And Downstream Produkte

Trimetrexate glucuronate Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

82952-64-5, Trimetrexate glucuronate Verwandte Suche:

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