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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 |
[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
| Related DNA/RNA Synthesis Products |
|---|
| Dencatistat
Dencatistat (P115) is an inhibitor of Cytidine Triphosphate Synthase 1 (CTPS1) with an IC50 value of ≤ 0.1 μM. |
| Antipain dihydrochloride
Antipain dihydrochloride is a protease inhibitor. Antipain dihydrochloride inhibits N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal aberrations. Antipain dihydrochloride also restricts uterine DNA synthesis and function in mice. |
| Tetrahydrouridine
Tetrahydrouridine (THU) is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine. |
| Crisnatol
Crisnatol (BWA770U) is a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol shows in vitro cytotoxicity against human breast cancer cells. Crisnatol (BWA770U) is also an orally active and anticancer agent. |
| Caf1-IN-1
Caf1-IN-1 is inhibitor for ribonuclease Caf1 with an IC50 of 0.59 µM. Caf1-IN-1 is also a weak inhibitor for poly(A)-specific ribonuclease (PARN) with IC50 of 23.9 µM. |
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