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2-[(3-氨基吡啶-2-基)亚甲基]氨基硫脲 /Triapine {[allProObj[0].p_purity_real_show]}

货号:A348408 同义名: 3-AP;PAN-811

Triapine is a ribonucleotide reductase inhibitor and a CDK inhibtor.

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Triapine 化学结构 CAS号:143621-35-6
Triapine 化学结构
CAS号:143621-35-6
Triapine 3D分子结构
CAS号:143621-35-6
Triapine 化学结构 CAS号:143621-35-6
Triapine 3D分子结构 CAS号:143621-35-6
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Triapine 纯度/质量文件 产品仅供科研

货号:A348408 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 DNA synthesis helicase RdRp ribonucleotide reductase tRNA synthetase YB-1 其他靶点 纯度
Fexinidazole 98%
Daptomycin 98%
Blasticidin S·HCl 98%
Metronidazole 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

98%
Triglycidyl isocyanurate p53 98+%
Nedaplatin 99%+
Bendamustine 98+%
Trifluridine 98%
Robinetin 99%+
Carboplatin 99%
Cidofovir 99%
Cisplatin 99%
Cytarabine ++++

DNA synthesis, IC50: 16 nM

98%
Acelarin ++++

DNA synthesis, EC50: 0.2 nM

99%+
Oxaliplatin 98%
YK-4-279 99%+
ML216 +

BLM636-1298, IC50: 0.97 μM

BLMfull-length, IC50: 2.98 μM

99%+
RK-33 98%
Brr2-IN-3 99%+
Phen-DC3 Trifluoromethanesulfonate 98%
Favipiravir 97%
Suramin sodium salt ++

RdRp, IC50: 0.26 μM

99%+
Clofarabine ++

Ribonucleotide reductase, IC50: 65 nM

97%
Didox 98%
(E)-3-AP 97%
Halofuginone +++

prolyl-tRNA synthetase, Ki: 18.3nM

99%+
BC-LI-0186 +++

Leucyl-tRNA synthetase, IC50: 46.11 nM

Leucyl-tRNA synthetase, Kd: 42.1 nM

98%
SU056 +

YB-1, IC50: 1.73 μM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Triapine 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].

Triapine 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
KBV1 cells Cytotoxicity assay 72 h Cytotoxicity against human P-glycoprotein-expressing KBV1 cells after 72 hrs by MTT assay, IC50=5.9 μM 19397322

Triapine 动物研究

Dose Mice: 10 mg/kg[3] (i.p.); 20 mg/kg[4] (s.c.)
Administration i.p., s.c.

Triapine 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 <<

Triapine 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

Triapine 实验方案

计算器
存储液制备 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

Triapine 技术信息

CAS号143621-35-6
分子式C7H9N5S
分子量 195.245
别名 3-AP;PAN-811;NSC663249. PAN-811;AIDS179996;3Apct;NSC 663249;3-Aminopyridine-2-Carboxyaldehyde Thiosemicarbazone;OCX191
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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

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