CI-898 (hydrochloride) (Synonyms: CI-898 trihydrochloride) |
| Catalog No.GC43267 |
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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1658520-97-8
Sample solution is provided at 25 µL, 10mM.
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CI-898 is a lipophilic antifolate inhibitor of dihydrofolate reductase (DHFR; Kds = 4.5, 1.4, and 0.1 nM for the bovine, murine, and E. coli enzyme, respectively). It has enhanced binding to DHFR in the presence of the cofactor NADPH (Kds = 0.03, 0.43, and 0.03 nM, respectively, for the bovine, murine, and E. coli enzyme). Cl-898 (30 nM) inhibits growth (IC50 = 20 nM after two days) and halts the cell cycle at the G1/S phase in L1210 mouse lymphocytic leukemia cells and is active against methotrexate-resistant cancer cell lines. It also inhibits the growth of S. faecalis and S. aureus when used at concentrations less than 0.25 μg/ml. In vivo, Cl-898 (0.44 mg/kg per day, p.o.) suppresses malarial effects in a mouse model of P. berghei infection and increases median survival time in a mouse model of T. gondii infection when administered at a dose of 180 mg/kg. It also enhances the activity of doxorubicin , cyclophosphamide , and 6-thioguanine in mice with advanced stage P338 leukemia.
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
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