Triapine is a potent ribonucleotide reductase inhibitor with broad spectrum antitumor activity by inhibiting DNA synthesis.
| Cell Experiment | |
|---|---|
| Cell lines | Wild-type KB and HU-resistant KB nasopharyngeal carcinoma cells. |
| Preparation method | Plating cells at a density of 104 cells/mL per well in 24-well plates. Adding drugs 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. |
| Concentrations | ~10 μM |
| Incubation time | A period of 3 generations |
| Animal Experiment | |
|---|---|
| Animal models | 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 | 0.9% NaCl or water |
| Dosages | ~24 mg/kg |
| Administration | i.p. or i.v. |
| Molecular Weight | 195.24 |
| Formula | C7H9N5S |
| CAS Number | 200933-27-3 |
| Solubility (25°C) | DMSO 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] William E Antholine, et al. Concentration of Fe(3+)-Triapine in BEAS-2B Cells
[5] Charles A Kunos, et al. Triapine Radiochemotherapy in Advanced Stage Cervical Cancer
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