141400-58-0|PX 12，≥98%|Medlife|Medlife为MCE，Selleck，麦克林，阿拉丁试剂，罗恩试剂，Sigma，安耐吉试剂，泰坦等同类产品品牌，上海现货，高性价比小分子化合物

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PX 12

PX-12(IV-2)是可逆的硫氧还蛋白-1（Trx-1）抑制剂; 抑制MCF-7 和HT-29 cells细胞生长的IC50值分别为1.9和2.9 μM。

目录号: PC10078 纯度: ≥98%

CAS No. :141400-58-0

商品编号	规格	价格	会员价
PC10078-10mg	10mg	¥686.00	请登录
PC10078-50mg	50mg	¥2646.00	请登录
PC10078-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥490.00	请登录

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中文名称

PX 12

中文别名

2-(仲丁基二硫基)-1H-咪唑;2-[(1-甲基丙基)二硫代]-1H-咪唑

英文名称

PX 12

英文别名

2-(sec-Butyldisulfanyl)-1H-imidazole;PX-12;1H-Imidazole,2-[(1-methylpropyl)dithio]-;PX 12;2-(butan-2-yldisulfanyl)-1H-imidazole;IV-2;MID;2-[(1-methylpropyl)dithio]-1H-imidazole;AK143053;2-((1-Methylpropyl)dithio)-1H-imidazole;1H-Imidazole, 2-[(1-methylpropyl)dithio]-;1H-Imidazole, 2-((1-methylpropyl)dithio)-;Iv 2 Compound;IV-2 compound;1-Methylpropyl-2-imidazolyl disulfide;PX12;C7H12N2S2;NOCA

Cas No.

141400-58-0

分子式

C₇H₁₂N₂S₂

分子量

188.31

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

PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1 (Trx-1); inhibits the growth of MCF-7 and HT-29 cells with IC₅₀ values of 1.9 and 2.9 μM, respectively.

性状

Solid

IC50 & Target[1][2]

IC50: 1.9 (MCF-7), 2.9 μM (HT-29 cells)

体外研究(In Vitro)

PX-12 inhibits the growth of MCF-7 and HT-29 cells with IC₅₀ values of 1.9 and 2.9 μM, respectively. PX-12 particularly reduces the activity of Trx-1 by means of thio-alkylating critical cysteine residue (Cys73) which is located in the outside the conserved redox catalytic site of Trx-1. PX-12 affects the oxidation state of thiols in a number of cell surface proteins. Key surface receptors for platelet adhesion and activation are affected, including the collagen receptor GPVI and the von Willebrand factor receptor, GPIb. PX-12 inhibits thrombus formation over Type I collagen in whole blood under flow conditions. Thioredoxin-1 (Trx-1) is a cellular redox protein that promotes tumor growth, inhibits apoptosis, and up-regulates hypoxia-inducible factor-1α and vascular endothelial growth factor. PX-12 inhibits the growth of colorectal cancer DLD-1 and SW620 cells in a dose- and time-dependent manner. PX-12 reduces cell colony formation and induced a G2/M phase arrest of the cell cycle. PX-12 treatment induces apoptosis. PX-12 inhibits colorectal cancer cell migration and invasion. Treatment of cancer cells with PX-12 reduces NOX1, CDH17 and S100A4 mRNA expression, and increases KLF17 mRNA expression. PX-12 decreases S100A4 protein expression in the colorectal cancer cells.

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

体内研究(In Vivo)

PX-12 has been shown to have in vivo antitumor activity against human tumor xenografts including HT-29 colon cancer in SCID mice and has been tested in a phase I clinical trial in patients.

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]. Welsh SJ, et al. The thioredoxin redox inhibitors 1-methylpropyl 2-imidazolyl disulfide and pleurotin inhibit hypoxia-induced factor 1alpha and vascular endothelial growth factor formation. Mol Cancer Ther. 2003 Mar;2(3):235-43. [Information]

[2]. Lou M, et al. Physical interaction between human ribonucleotide reductase large subunit and thioredoxin increases colorectal cancer malignancy. J Biol Chem. 2017 Jun 2;292(22):9136-9149. [Information]

[3]. Metcalfe C, et al. Thioredoxin Inhibitors Attenuate Platelet Function and Thrombus Formation. PLoS One. 2016 Oct 7;11(10):e0163006 [Information]

[4]. Ramanathan RK, et al. A Phase I pharmacokinetic and pharmacodynamic study of PX-12, a novel inhibitor of thioredoxin-1, in patients with advanced solid tumors. Clin Cancer Res. 2007 Apr 1;13(7):2109-14. [Information]

[5]. Wang F, et al. Thioredoxin-1 inhibitor, 1-methylpropyl 2-imidazolyl disulfide, inhibits the growth, migration and invasion of colorectal cancer cell lines. Oncol Rep. 2015 Feb;33(2):967-73. [Information]

溶解度数据

体外研究:

Ethanol : 50 mg/mL (265.52 mM; Need ultrasonic)

DMSO : ≥ 44.7 mg/mL (237.37 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	5.3104 mL	26.5520 mL	53.1039 mL
5 mM	1.0621 mL	5.3104 mL	10.6208 mL
10 mM	0.5310 mL	2.6552 mL	5.3104 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 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (13.28 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (13.28 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
2.

建议依照次序添加每种溶剂： 10% EtOH 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (13.28 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (13.28 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 EtOH 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
3.

建议依照次序添加每种溶剂： 10% EtOH 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (13.28 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (13.28 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 EtOH 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
4.

建议依照次序添加每种溶剂： 10% EtOH 90% corn oil
Solubility: ≥ 2.5 mg/mL (13.28 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (13.28 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL玉米油中，混合均匀。

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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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