product name Triapine
Description: Triapine (also known as 3-AP) is a potent ribonucleotide reductase inhibitor with broad spectrum antitumor activity by inhibiting DNA synthesis. In addition, Triapine has been revealed to inhibit the growth of the murine M109 lung carcinoma and human A2780 ovarian carcinoma xenografts in nude mice. Moreover, Triapine was active against the L1210 leukemia over a broad range of dosages and was curative for the M109 lung carcinoma and human A2780 ovarian carcinoma xenograft mice.
References: Biochem Pharmacol. 2000 Apr 15;59(8):983-91; CNS Drug Rev. 2006 Spring;12(1):77-90.
195.24
Formula
C7H9N5S
CAS No.
200933-27-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 20 mg/mL (102.4 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
4% DMSO+dd H2O: 10mg/mL
Synonyms
3-AP
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/1941208
| In Vitro |
In vitro activity: Triapine potently inhibits the activity of ribonucleotide reductase in both wild-type KB and HU-resistant KB nasopharyngeal carcinoma cells. Triapine shows broad spectrum antitumor activity by inhibiting DNA synthesis in a series of cancer cell lines. In vitro, Triapine blocks ischemic neurotoxicity and hypoxic toxicity with EC50 of 0.35 μM and 0.75 μM, respectively. Triapine also shows its neuroprotective activity by suppressing cell death induced by neurotoxic agents, including staurosporine, veratridine and glutamate. Kinase Assay: CDP reductase is assayed using Dowex 1-borate ion-exchange chromatography. The assay mixture contains 0.02 μCi of [14C]CDP (52.9 mCi/mmol), 3 mM dithiothreitol, 6 mM MgCl2, 30 mM HEPES, 5 mM ATP, 0.15 mM unlabeled CDP, and 10 μL of cellular extract in a final volume of 0.02 mL. The incubation time for the reaction is 60 min, during which time the reaction is linear. Cell Assay: Cells (Wild-type KB and HU-resistant KB nasopharyngeal carcinoma cells.) are plated at a density of 104 cells/mL per well in 24-well plates. Drugs are added to cells and incubations are continued for a period of 3 generations (untreated control cells), followed by assessment of cell growth by the methylene blue assay. |
|---|---|
| In Vivo | In mice bearing the L1210 leukemia, Triapine (1.25 to 20 mg/kg) is curative for some mice without lethal toxicity. Triapine also inhibits the growth of solid tumors in mice M109 lung carcinoma and human A2780 ovarian carcinoma xenografts. In addition, combination of Triapine with various classes of agents that damage DNA results in synergistic inhibition of the L1210 leukemia. In a rat model of transient ischemia, Triapine reduces infarct volume by 59% when administered i.c.v. (50 μ per rat) and by 35% when administered i.v. (1 mg/kg). |
| Animal model | BALB/cBA/2 (CD2F1) mice with the L1210 leukemia and the M109 lung carcinoma, athymic nu/nu mice with the human A2780 ovarian carcinoma xenograft. |
| Formulation & Dosage | Dissolved in 0.9% NaCl or water; 24 mg/kg; i.p. or i.v. |
| References | Biochem Pharmacol. 2000 Apr 15;59(8):983-91; CNS Drug Rev. 2006 Spring;12(1):77-90. |
