3-AP
(Synonyms: [(3-氨基吡啶-2-基)亚甲基氨基]硫脲,3-Aminopyridine-2-Carboxyaldehyde Thiosemicarbazone,NSC 663249,Triapine?) 目录号 : GC13510
A ribonucleotide reductase inhibitor
Cas No.:143621-35-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | An MTT assay is used to determine cell growth inhibition of CHO cells. Human leukemia K562 cells and K/VP.5 cells (a 26-fold etoposide-resistant K562-derived sub-line with decreased levels of topoisomerase IIα mRNA and protein) are maintained as suspension cultures in MEM containing 10% fetal calf serum (FCS). For growth inhibition assays, K562 and K/VP.5 cells are plated at a concentration of 1.5×105 cell/mL, and incubated 5 d with various concentrations of Dp44mT, 3-AP or vehicle (DMSO) for 48 h, after which cells are counted on a model ZBF Coulter counter. The IC50 growth inhibitory concentration for each cell line is calculated from a non-linear least-squares fit to a 2-parameter logistic equation[2]. |
Animal experiment: | Mice[3]Female BALB/c nu/nu mice are used at 8-10 weeks of age. Tumor cells in culture are harvested, and 107 cells are suspended in Matrigel and injected s.c. into the right flanks of mice. After engraftment, tumor size is measured by Vernier calipers. Tumor volumes (in cubic millimeters) are calculated. When tumor volumes reached 120 mm3, i.v. treatment began (day 0). Chelators (e.g., 3-AP) are dissolved in 15% propylene glycol in 0.9% saline and injected i.v. over 5 consecutive days per week for up to 7 weeks. Control mice are treated with vehicle alone. |
References: [1]. Martin LK, et al. A dose escalation and pharmacodynamic study of Triapine and radiation in patients with locally advanced pancreas cancer. Int J Radiat Oncol Biol Phys. 2012 Nov 15;84(4):e475-81. | |
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.
| Cas No. | 143621-35-6 | SDF | |
| 别名 | [(3-氨基吡啶-2-基)亚甲基氨基]硫脲,3-Aminopyridine-2-Carboxyaldehyde Thiosemicarbazone,NSC 663249,Triapine? | ||
| 化学名 | 2-[(3-amino-2-pyridinyl)methylene]-hydrazinecarbothioamide | ||
| Canonical SMILES | NC(N/N=C/C1=C(N)C=CC=N1)=S | ||
| 分子式 | C7H9N5S | 分子量 | 195.2 |
| 溶解度 | ≤20mg/ml in DMSO;25mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 5.123 mL | 25.6148 mL | 51.2295 mL |
| 5 mM | 1.0246 mL | 5.123 mL | 10.2459 mL |
| 10 mM | 0.5123 mL | 2.5615 mL | 5.123 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。