Bioactivity | 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]. |
Invitro | Trimetrexate isethionate (0.1 μM; 18 h) completely inhibits proliferation of toxoplasma in murine macrophages[3].Trimetrexate isethionate (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]. Cell Proliferation Assay[5] Cell Line: |
Name | Trimetrexate isethionate |
CAS | 82935-04-4 |
Formula | C21H29N5O7S |
Molar Mass | 495.55 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |