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Triapine

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Chemical Structure| 143621-35-6 同义名 : 3-AP;PAN-811;NSC663249. PAN-811;AIDS179996;3Apct;NSC 663249;3-Aminopyridine-2-Carboxyaldehyde Thiosemicarbazone;OCX191
CAS号 : 143621-35-6
货号 : A348408
分子式 : C7H9N5S
纯度 : 99%+
分子量 : 195.245
MDL号 : MFCD00924747
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 45 mg/mL(230.48 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

5%DMSO+40%PEG300+5%Tween80+50%water 1.25 mg/mL

生物活性
描述 Ribonucleotide reductase catalyzes the formation of deoxyribonucleotides from ribonucleotides, which is essential for maintaining a balanced pool of deoxyribonucleotides for DNA synthesis and repair. Triapine is a potent inhibitor of ribonucleotide reductase. In vitro, it fully blocked ischemic neurotoxicity at 0.5 μM with an EC50 value of 0.35 μM. It also inhibited hypoxic toxicity with an EC50 value of around 0.75 μM. Triapine at 0.63 μM and 0.45 μM completely inhibited HGH-induced mitochondrial dysfunction and LDH release with EC50 values of 0.2 - 0.35 μM. In neuron cells, treatment with 10 μM Triapine decreased 100 μM glutamate-induced cell death by 89%. In cortical neurons, the addition of 10 μM Triapine 24h prior to and during the experiment reduced neurotoxicity of 1 μM staurosporine by 47%Jiang ZG, Lebowitz MS, Ghanbari HA. Neuroprotective activity of 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (PAN-811), a cancer therapeutic agent. CNS Drug Rev. 2006 Spring;12(1):77-90. doi: 10.1111/j.1527-3458.2006.00077.x. PMID: 16834759; PMCID: PMC6741723.https://pubmed.ncbi.nlm.nih.gov/16834759/. In mice bearing M109 lung carcinoma, intravenous injection of triapine either once daily (24 mg/kg) or twice daily (6 mg/kg) for 5 consecutive days significantly inhibited the tumor growth. The administration of triapine (5 mg/kg, twice daily, 5 consecutive days) also inhibited the DNA synthesis in the bone marrow and intestinal mucosa[5].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
HCT116 cells 4 μM Function assay 24 h Induction of ROS generation in human HCT116 cells expressing wild type p53 at 4 uM after 24 hrs by spectrophotometry 24900837
human HCT116 cells Cytotoxicity assay 96 h Dark cytotoxicity against human HCT116 cells expressing wild type p53 after 96 hrs by MTT assay, IC50=1.226 μM 24900837
KB-3-1 cells Cytotoxicity assay 72 h Cytotoxicity against human P-gp-negative KB-3-1 cells after 72 hrs by MTT assay, IC50=1.4 μM 19397322
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02644122 - Terminated(Slow enrollment) - -
NCT02644122 Metastatic Squamous Neck Cance... 展开 >>r With Occult Primary Squamous Cell Carcinoma 收起 << Phase 2 Terminated(Slow enrollment) - United States, California ... 展开 >> UC San Diego Moores Cancer Center La Jolla, California, United States, 92093 收起 <<
NCT00024323 Unspecified Adult Solid Tumor,... 展开 >> Protocol Specific 收起 << Phase 1 Completed - United States, Arizona ... 展开 >> Arizona Clinical Research Center Tucson, Arizona, United States, 85712 United States, Connecticut Yale Comprehensive Cancer Center New Haven, Connecticut, United States, 06520-8028 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.12mL

1.02mL

0.51mL

25.61mL

5.12mL

2.56mL

51.22mL

10.24mL

5.12mL
参考文献

[1]Jiang ZG, Lebowitz MS, Ghanbari HA. Neuroprotective activity of 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (PAN-811), a cancer therapeutic agent. CNS Drug Rev. 2006 Spring;12(1):77-90.

[2]Finch RA, Liu M, et al. Triapine (3-aminopyridine-2-carboxaldehyde- thiosemicarbazone): A potent inhibitor of ribonucleotide reductase activity with broad spectrum antitumor activity. Biochem Pharmacol. 2000 Apr 15;59(8):983-91.

[3]Lin ZP, Zhu YL, et al. Combination of triapine, olaparib, and cediranib suppresses progression of BRCA-wild type and PARP inhibitor-resistant epithelial ovarian cancer. PLoS One. 2018 Nov 16;13(11):e0207399.

[4]Dai L, Chen J, et al. Ribonucleotide Reductase Inhibitor 3-AP Induces Oncogenic Virus Infected Cell Death and Represses Tumor Growth. J Cancer. 2018 Oct 31;9(23):4503-4509.

[5]10692563