3-AP|143621-35-6|(3-AP; PAN-811; OCX191)-陌孚医药/Medlife

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3-AP (Synonyms: 3-AP; PAN-811; OCX191)

目录号: PC15363 纯度: ≥98%

CAS No. :143621-35-6

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中文名称

3-AP

中文别名

2-[(3-氨基吡啶-2-基)亚甲基]氨基硫脲;(3-氨基吡啶-2-基)亚甲基氨基]硫脲;[(3-氨基吡啶-2-基)亚甲基氨基]硫脲

英文名称

3-AP

英文别名

2-((3-Aminopyridin-2-yl)methylene)hydrazinecarbothioamide;2-[(3-Aminopyridin-2-yl)methylene]hydrazinecarbothioamide;3-AP;Hydrazinecarbothioamide,2-[(3-amino-2-pyridinyl)methylene]-;TRIAPINE;3-Am;3-amino-2-carboxaldehyde-pyridine thiosemicarbazone;3-aminopyridine hydrochloride;3-aminopyridine-2-carbaldehyde thiosemicarbazone;3-aminopyridine-2-carboxaldehydethiosemicarbazone;3-aminopyridinium hydrochloride;3-Pyridinamine hydrochloride;AC1MHQ7Y;CTK3I9491;NSC663249;OCX191;PAN-811;pyridin-3-amine hydrochloride;Pyridine, 3-amino-, hydrochloride;SureCN3365191;OCX 0191;Pan 811;3-Apct;3-Aminopyridine-2-carboxaldehyde thiosemicarbazone;OCX 191;C7H9N5S;U4XIL4091C;3-aminopyridine-2-carbaldehyde-thiosemicarbazone;[(E)-(3-amino-2-pyridyl)methyleneamino]thiourea;Hydrazinecarbothioamide, 2-((3-amino-2-pyridinyl)methylene)-;(E)-2-((3-aminopyridin-2-yl)methylene)hydrazinecarbothioamide;PAN811;AK120530;[(3-aminopyridin

Cas No.

143621-35-6

分子式

C₇H₉N₅S

分子量

195.24

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

3-AP (PAN-811) is a potent inhibitor of the M2 subunit of ribonucleotide reductase (RR), and is a potent radiosensitizer.

性状

Solid

IC50 & Target[1][2]

Ribonucleotide reductase (RR)

体外研究(In Vitro)

3-AP (Triapine) is a potent derivative of α-heterocyclic carboxaldehyde thiosemicarbazone (HCT) that inhibits hRRM2 and p53R2 isoforms of the M2 subunit. 3-AP (Triapine) is thought to inhibit ribonucleotide reductase through its preformed iron chelate, rather than directly by removing iron from the active site. In cells containing less topoisomerase IIα fewer DNA strand breaks will be produced, and thus topoisomerase II poisons will be less inhibitory in the K/VP.5 cell line. The IC₅₀s for Dp44mT growth inhibition are 48±9 nM and 60±12 nM, for K562 and K/VP.5 cells, respectively. The IC₅₀s for 3-AP growth inhibition are 476±39 nM and 661±69 nM for K562 and K/VP.5 cells, respectively. PKIH and DpT Fe chelators show high antiproliferative activity against a range of tumor cell lines. Dp44mT shows the greatest antitumor efficacy with an IC₅₀ that ranged from 0.005 to 0.4 μM. The average IC₅₀ of Dp44mT over 28 cell types is 0.03±0.01 μM, which is significantly lower than that of 3-AP (Triapine; average IC₅₀: 1.41±0.37 μM).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

3-AP (Triapine) causes a significant increase (1.7-fold) in splenic weight when expressed as a percentage of total body weight (1.02±0.06%; n=25) compared with control mice (0.6±0.03%; n=27). In the long-term group, a significant increase in heart weight is observed after Dp44mT (0.4 mg/kg per day) (0.8±0.06%; n=4) compared with control mice (0.5±0.01%; n=6). A significant decrease in the expression of Ndrg1, TfR1, and VEGF1 in the liver is noted for Dp44mT- and 3-AP (12 mg/kg per day)-treated animals. The decreased expression could be related to the increased liver Fe in both Dp44mT- and 3-AP-treated mice.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[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. [Information]

[2]. Yalowich JC, et al. The anticancer thiosemicarbazones Dp44mT and Triapine lack inhibitory effects as catalytic inhibitors or poisons of DNA topoisomerase IIα. Biochem Pharmacol. 2012 Jul 1;84(1):52-8. [Information]

[3]. Whitnall M, et al. A class of iron chelators with a wide spectrum of potent antitumor activity that overcomes resistance to chemotherapeutics. Proc Natl Acad Sci U S A. 2006 Oct 3;103(40):14901-6. [Information]

溶解度数据

体外研究:

DMSO : ≥ 47 mg/mL (240.73 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	5.1219 mL	25.6095 mL	51.2190 mL
5 mM	1.0244 mL	5.1219 mL	10.2438 mL
10 mM	0.5122 mL	2.5610 mL	5.1219 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (12.80 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (12.80 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (12.80 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (12.80 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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