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Submit ReviewCI 898 trihydrochloride
Discontinued Product
CI 898 trihydrochloride (Cat. No. 2039) has been withdrawn from sale for commercial reasons.
Description: Dihydrofolate reductase inhibitor
Alternative Names: TMTX, Trimetrexate
Chemical Name: 5-Methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine trihydrochloride
Purity: ≥95% (HPLC)
Biological Activity
Potent lipophilic inhibitor of dihydrofolate reductase (DHFR) that displays antineoplastic and antiprotozoal properties. Inhibits protozoal, bacterial and human DHFR with IC50 values of 1.4, 6.1 and 3.2 nM respectively. Affects G1/S phase cell cycle progression.
Technical Data
| M. Wt | 478.8 |
| Formula | C19H23N5O3.3HCl |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 1658520-97-8 |
| PubChem ID | 45006154 |
| Smiles | NC1=NC(N)=NC(C=C3)=C1C(C)=C3CNC2=CC(OC)=C(OC)C(OC)=C2.Cl.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets
References
References are publications that support the biological activity of the product.
Hook et al (1986) Cell cycle effects of trimetrexate (CI-898). Cancer Chemother.Pharmacol. 16 116 PMID: 2936525
Chan and Anderson (2006) Towards species-specific antifolates. Curr.Med.Chem. 13 377 PMID: 16475929
Allegra et al (1987) Potent in vitro and in vivo antitoxoplasma activity of the lipid-soluble antifolate trimetrexate. J.Clin.Invest. 79 478 PMID: 2948969
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1 Citation for CI 898 trihydrochloride
Citations are publications that use Tocris products. Selected citations for CI 898 trihydrochloride include:
Sienkiewicz et al (2008) Chemical and genetic validation of dihydrofolate reductase-thymidylate synthase as a drug target in African trypanosomes. Mol Microbiol 69 520 PMID: 18557814
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