Trimetrexate trihydrochloride (Synonyms: CI-898 trihydrochloride)

Cat. No.: HY-10373A: FAQs
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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.

For research use only. We do not sell to patients.

Trimetrexate trihydrochloride Chemical Structure

CAS No. : 1658520-97-8

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Other In-stock Forms of Trimetrexate trihydrochloride:

Trimetrexate

Other Forms of Trimetrexate trihydrochloride:

1 Publications Citing Use of MCE Trimetrexate trihydrochloride

•Sci Data. 2024 Sep 19.

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target^[1]

Toxoplasma

In Vitro

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.

Cell Proliferation Assay^[5]

Cell Line:	SNU-C4 and NCI-H630
Concentration:	0.1 mM
Incubation Time:	24 h
Result:	Inhibited cell growth by 50-60% in both cell lines.

Cell Proliferation Assay^[5]

Cell Line:	C4 cells
Concentration:	1 and 10 mM
Incubation Time:	24 h
Result:	Produced 42% and 50% lethality at 1 and 10 mM, respectively.

In Vivo

Trimetrexate (180 mg/kg or 30 mg/kg; p.o. or i.p.; daily) trihydrochloride extends the median survival of the toxoplasma infected mice and shows antitoxoplasma activity^[3]. Trimetrexate (0-30 mg/kg; i.v.; once daily for 5days) trihydrochloride shows chronic toxicity in rats^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Toxoplasma infected female BALB/c mice weighing about 20 g^[3]
Dosage:	180 mg/kg or 30 mg/kg
Administration:	180 mg/kg per day orally in the drinking water or 30 mg/kg per day i.p.
Result:	Extended the median survival of the infected mice to 10 d (p.o.) or 19 d (i.p.).

Animal Model:	Charles River Wistar Crl(WI)BR rats weighing approximately 150 to 200 g^[4]
Dosage:	0, 1, 10, or 30 mg/kg
Administration:	Intravenous injection, once daily for 5 consecutive days followed by a 23-day recovery period
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.

Clinical Trial

Molecular Weight

478.80

Formula

C₁₉H₂₆Cl₃N₅O₃

CAS No.

1658520-97-8

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

Trimetrexate trihydrochloride Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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