Triapine (3-AP)

Cell lines

Wild-type (KB) and HU-resistant (KB/HU) human KB nasopharyngeal carcinoma cells.

Preparation method

The solubility of this compound in DMSO is > 83.3 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

37oC

Applications

Triapine is found to be a much more potent inhibitor of the enzyme than HU regardless of the cellular source of the enzyme, with a comparable inhibition at roughly a 1000-old lower concentration of Triapine than HU.

Animal models

Mice xenografts of murine M109 lung carcinoma and the human A2780 ovarian carcinoma.

Dosage form

i.p. or i.v. bolus injection (0.01 mL/g)

Preparation method

Triapine in 0.9% NaCl

Applications

Triapine significantly inhibits the growth in mice of the M109 lung carcinoma, the twice daily schedule produces tumor growth delays of 10 days compared to untreated control animals. Growth of the human A2780 ovarian carcinoma xenograft in nude mice is also significantly inhibited by Triapine, at 8 and 10 mg/kg given on a twice daily schedule.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1. Finch RA, Liu M, Grill SP et al. Triapine (3-aminopyridine-2-carboxaldehyde- thiosemicarbazone): A potent inhibitor of ribonucleotide reductase activity with broad spectrum antitumor activity. Biochem Pharmacol. 2000 Apr 15;59(8):983-91.