82935-04-4
Chemical Structure
Trimetrexate isethionate
Synonym(s): CI-898 isethionate
- CAS No.: 82935-04-4
- Formula:C21H29N5O7S
- Molecular Weight:495.55
IUPAC Name: 5-methyl-6-(((3,4,5-trimethoxyphenyl)amino)methyl)quinazoline-2,4-diamine 2-hydroxyethane-1-sulfonate
InChIKey: YATKEMOVGUXIDY-UHFFFAOYSA-N
SMILES: OCCS(=O)(O)=O.NC1=NC(N)=C2C(C)=C(CNC3=CC(OC)=C(OC)C(OC)=C3)C=CC2=N1
Biological Activity: Trimetrexate (CI-898) isethionate 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 isethionate can also inhibit the growth of various cancer cells. Trimetrexate isethionate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer[1][2][3][4][5].
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Trimetrexate isethionate | Trimetrexate (CI-898) isethionate 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 isethionate can also inhibit the growth of various cancer cells. Trimetrexate isethionate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer. | |||||||||||||||||||||
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- [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]
Keywords
