| CAS NO: | 143621-35-6 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 195.2 |
| Cas No. | 143621-35-6 |
| Formula | C7H9N5S |
| Synonyms | 3-Aminopyridine-2-Carboxyaldehyde Thiosemicarbazone,NSC 663249,Triapine(TM) |
| Solubility | ≤20mg/ml in DMSO;25mg/ml in dimethyl formamide |
| Chemical Name | 2-[(3-amino-2-pyridinyl)methylene]-hydrazinecarbothioamide |
| Canonical SMILES | NC(N/N=C/C1=C(N)C=CC=N1)=S |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
3-AP is a ribonucleotide reductase inhibitor and iron chelator with antitumor activity.
Ribonucleotide reductase, the rate-limiting enzyme for de novo DNA synthesis, is an excellent target for chemotherapy. The increased activity of ribonucleotide reductase in cancer cells has been reported to be associated with malignant proliferation and transformation.
In vitro: Previous study found that the exposure of the tumor cell lines to 3-AP before or immediately after irradiation resulted in an increase in radiosensitivity. In contrast, 3-AP could enhance the radiosensitivity of the normal fibroblast cell line only when the exposure was before irradiation. There were no consistent differences between cell lines with respect to the expression of the RR subunits. Whereas 3-AP had no effect on radiation-induced gammaH2AX foci at 1 hour, the number of gammaH2AX foci per cell was significantly greater in the 3-AP-treated cells at 24 hours after irradiation, demonstrating the presence of unrepaired DNA damage [1].
In vivo: Animal study found that 3-AP administration to mice bearing tumor xenografts immediately after irradiation led to a greater than additive increase in radiation-induced tumor growth delay [1].
Clinical trial: Clinical study shows that triapine radiochemotherapy was safe, active, and effective in patients with untreated advanced-stage cervical cancer, worthy of randomized clinical trial study [2].
References:
[1] Barker, C. A.,Burgan, W.E.,Carter, D.J., et al. In vitro and in vivo radiosensitization induced by the ribonucleotide reductase inhibitor triapine (3-aminopyridine-2-carboxaldehyde-thiosemicarbazone). Clinical Cancer Research 12(9), 2912-2918 (2006).
[2] Kunos CA, Sherertz TM. Long-Term Disease Control with Triapine-Based Radiochemotherapy for Patients with Stage IB2-IIIB Cervical Cancer. Front Oncol. 2014 Jul 24;4:184.
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