CI 898 trihydrochloride

Discontinued Product

Unfortunately CI 898 trihydrochloride (Cat. No. 2039) has been withdrawn from sale for commercial reasons.
Cat.No. 2039 - CI 898 trihydrochloride | C19H23N5O3.3HCl | CAS No. 1658520-97-8
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)
Citations (1)

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.

All Tocris products are intended for laboratory research use only.

Preparing Stock Solutions

The following data is based on the product molecular weight 478.8. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.09 mL 10.44 mL 20.89 mL
5 mM 0.42 mL 2.09 mL 4.18 mL
10 mM 0.21 mL 1.04 mL 2.09 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References are publications that support the products' biological activity.

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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