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Trimetrexate

Trimetrexate Struktur
52128-35-5
CAS-Nr.
52128-35-5
Englisch Name:
Trimetrexate
Synonyma:
CI-898;NSC249008;NSC-249008;Trimetrexate;CI-898; CI 898; CI898;CI-898;NSC-249008;CI898;NSC249008;5-Methyl-6-(3,4,5-trimethoxyanilinomethyl)quinazoline-2,4-diamine;5-Methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine;5-Methyl-6-{[(3,4,5-triMethoxyphenyl)aMino]Methyl}quinazoline-2,4-diaMine;2,4-Quinazolinediamine, 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-
CBNumber:
CB31075279
Summenformel:
C19H23N5O3
Molgewicht:
369.42
MOL-Datei:
52128-35-5.mol

Trimetrexate Eigenschaften

Schmelzpunkt:
215-217 °C
Siedepunkt:
647.0±65.0 °C(Predicted)
Dichte
1.305±0.06 g/cm3(Predicted)
storage temp. 
2-8°C(protect from light)
L?slichkeit
DMSO : ≥ 61.5 mg/mL (166.48 mM)
Aggregatzustand
Solid
pka
8.09±0.30(Predicted)
Farbe
Light yellow to green yellow
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Warnung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H302 Gesundheitssch?dlich bei Verschlucken. Akute Toxizit?t oral Kategorie 4 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P270, P301+P312, P330, P501
H315 Verursacht Hautreizungen. Hautreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P302+P352, P321,P332+P313, P362
H319 Verursacht schwere Augenreizung. Schwere Augenreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P305+P351+P338,P337+P313P
H335 Kann die Atemwege reizen. Spezifische Zielorgan-Toxizit?t (einmalige Exposition) Kategorie 3 (Atemwegsreizung) Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" />
Sicherheit
P261 Einatmen von Staub vermeiden.
P305+P351+P338 BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen.

Trimetrexate Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Trimetrexate (TMQ) has been approved for the treatment of Pneumocystis carinii in patients with AIDS and also exhibits antiprotozoal activity against Trypanosoma cruzi . The drug is available as a single-ingredient medication, but it can be administered along with folinic acid in much the same way that methotrexate is administered with calcium leucovorin in cancer chemotherapy. Trimetrexate is a derivative of methotrexate.

Verwenden

Trimetrexate is an FDA-approved drug which selectively inhibits Streptococcus mutans through targeting dihydrofolate reductase (DHFR).

Allgemeine Beschreibung

The drug is available as a lyophilized powder in 5- or 30-mgvials for IV use. The drug is used to treat colorectal cancer,head and neck cancer as well as NSCLC. The mechanism ofaction of trimetrexate involves folate antagonism and inhibitionof thymidylate synthesis. Trimetrexate does not formintracellular polyglutamate adducts as does methotrexateand other related compounds. Resistance can occur by increasedexpression of the target enzyme, decreased bindingaffinity for the target enzyme, or decreased intracellulardrug transport. Trimetrexate is administered only by the IVroute and distributed throughout the body with extensivebinding to plasma proteins. The major catabolic pathwaysinvolve O-demethylation followed by glucuronide conjugation.The drug interaction and toxicity profiles are similar tothose for methotrexate.

Mechanism of action

Trimetrexate is considered to be a nonclassical folate antagonist, whereas methotrexate, the structurally similar analogue of TMQ, is a classical folate antagonist. The difference between these two drugs is that methotrexate, with its polar glutamate side chain, is transported into the cell via a carrier-mediated transport system, whereas TMQ, without the glutamate moiety, is absorbed by the cell via a passive diffusion. Once in the cell, TMQ inhibits DHFR. Trimetrexate binds to Pneumocystis cari nii DHFR 1,500 times more strongly than trimethoprim and somewhat more strongly than methotrexate. It also has been reported that TMQ readily enters the P. carinii cell because of the lipophilic nature of this drug. Methotrexate and leucovorin are not able to enter the cell, however, because the cell membrane of P. carinii does not possess the transporter protein.

Clinical Use

Trimetrexate, when combined with the cytoprotective agent leucovorin, is more effective and better tolerated than pentamidine in the treatment of PCP. Because the first- and second-line agents are successful in only 50 to 75% of these cases, and because adverse reactions severely limit the use of some of the older agents, TMQ may offer some advantages in treatment. Trimetrexate is administered by IV infusion over 60 to 90 minutes and should be combined with the cytoprotective drug leucovorin. The leucovorin protects against bone marrow suppression and against renal and hepatic dysfunction. Leucovorin administration should continue for 72 hours after the last dose of TMQ. Additionally, TMQ has been reported to be effective in the treatment of Chagas' disease.

Trimetrexate Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Trimetrexate Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 40)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Shaanxi Dideu Medichem Co. Ltd
+86-29-87569266 15319487004
1015@dideu.com China 4087 58
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000
marketing@targetmol.com United States 32077 58
Baoji Guokang Bio-Technology Co., Ltd.
0917-3909592 13892490616
gksales1@gk-bio.com China 9315 58
Shanghai Acmec Biochemical Technology Co., Ltd.
+undefined18621343501
product@acmec-e.com China 33338 58
TargetMol Chemicals Inc.
+8613564774135
zijue.cai@tsbiochem.com United States 19863 58
SHANGHAI KEAN TECHNOLOGY CO., LTD.
+8613817748580
cooperation@kean-chem.com China 40066 58
Amadis Chemical Company Limited
571-89925085
sales@amadischem.com China 131957 58
LGM Pharma 1-(800)-881-8210
inquiries@lgmpharma.com United States 2123 70
Beijing HuaMeiHuLiBiological Chemical 010-56205725
waley188@sohu.com China 12335 58
ShangHai Caerulum Pharma Discovery Co., Ltd. 18149758185 18149758185
sales-cpd@caerulumpharma.com China 3466 58

52128-35-5()Verwandte Suche:


  • Trimetrexate
  • 5-Methyl-6-(3,4,5-trimethoxyanilinomethyl)quinazoline-2,4-diamine
  • 5-Methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine
  • CI-898
  • 2,4-Quinazolinediamine, 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-
  • 5-Methyl-6-{[(3,4,5-triMethoxyphenyl)aMino]Methyl}quinazoline-2,4-diaMine
  • NSC249008
  • CI-898; CI 898; CI898
  • CI-898;NSC-249008;CI898;NSC249008
  • NSC-249008
  • 52128-35-5
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