Trimetrexate trihydrochloride
Based on 3 publication(s) in Google Scholar
Trimetrexate (CI-898) trihydrochloride is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate trihydrochloride can also inhibit the growth of various cancer cells. Trimetrexate trihydrochloride can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer.
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- CAS No.: 1658520-97-8
- Formule: C19H26Cl3N5O3
- Masse moléculaire:478.80
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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Toxoplasma |
Trimetrexate trihydrochloride (0.1 μM, 18 h) completely inhibits proliferation of toxoplasma in murine macrophages[3].
Trimetrexate trihydrochloride (1 μM) can cross the toxoplasma cell membrane and rapidly reaches high intracellular concentrations (108 pmol/107 cells within 10 min) [3].
Trimetrexate (0.1 mM; 24 h) inhibits cell growth by 50-60% in SNU-C4 and NCI-H630 cell lines[5].
Trimetrexate (1 and 10 mM; 24 h) produces lethality and inhibits DHFR in C4 cells[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SNU-C4 and NCI-H630
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Concentration:0.1 mM
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Incubation Time:24 h
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Result:Inhibited cell growth by 50-60% in both cell lines.
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Cell Line:C4 cells
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Concentration:1 and 10 mM
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Incubation Time:24 h
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Result:Produced 42% and 50% lethality at 1 and 10 mM, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Toxoplasma infected female BALB/c mice weighing about 20 g[3]
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Dosage:180 mg/kg or 30 mg/kg
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Administration:180 mg/kg per day orally in the drinking water or 30 mg/kg per day i.p.
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Result:Extended the median survival of the infected mice to 10 d (p.o.) or 19 d (i.p.).
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Animal Model:Charles River Wistar Crl(WI)BR rats weighing approximately 150 to 200 g[4]
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Dosage:0, 1, 10, or 30 mg/kg
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Administration:Intravenous injection, once daily for 5 consecutive days followed by a 23-day recovery period
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Result:Showed chronic toxicity, the testicular changes persisting during the course of multiple cycles of dosing were not reversible within 21 days, but required an additional 56 days for essentially complete recovery.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1658520-97-8
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Masse moléculaire 478.80
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Formule C19H26Cl3N5O3
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SMILES
NC1=C(C(C)=C2CNC3=CC(OC)=C(OC)C(OC)=C3)C(C=C2)=NC(N)=N1.[H]Cl.[H]Cl.[H]Cl
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Synonyms
CI-898 trihydrochloride
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Commun
IQGAP3 bridges matrix stiffness with glioma stem cell maintenance and radioresistance by stabilizing SOX2. [Abstract]2026 Jun 6. PMID: 42251046 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
Antimicrob Agents Chemother
Multidrug tolerance conferred by loss-of-function mutations in anti-sigma factor RshA of Mycobacterium abscessus. [Abstract]2024 Dec 5;68(12):e0105124. PMID: 39470195
Pureté et documentation
Références
[1]. Hopper AT, et al. Discovery of Selective Toxoplasma gondii Dihydrofolate Reductase Inhibitors for the Treatment of Toxoplasmosis. J Med Chem. 2019 Feb 14;62(3):1562-1576. [Content Brief]
[2]. Fulton, B., et al. Trimetrexate. Drugs 49, 563–576 (1995). [Content Brief]
[3]. Allegra CJ, et al. Potent in vitro and in vivo antitoxoplasma activity of the lipid-soluble antifolate trimetrexate. J Clin Invest. 1987 Feb;79(2):478-82. [Content Brief]
[4]. Dethloff LA, et al. Chronic toxicity of the anticancer agent trimetrexate in rats. Fundam Appl Toxicol. 1992 Jul;19(1):6-14. [Content Brief]
[5]. Grem JL, Voeller DM, Geoffroy F, Horak E, Johnston PG, Allegra CJ. Determinants of trimetrexate lethality in human colon cancer cells. Br J Cancer. 1994 Dec;70(6):1075-84. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Trimetrexate trihydrochloride Related Classifications
HY-10373A Related Classifications
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