Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PX-12 (PX12) 是一种可逆的硫氧还蛋白-1(Trx-1)抑制剂,能够抑制 MCF-7 细胞(IC50:1.9 μM)和HT-29 细胞(IC50:2.9 μM)的生长。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 178 | 现货 | ||
5 mg | ¥ 455 | 现货 | ||
10 mg | ¥ 647 | 现货 | ||
25 mg | ¥ 1,230 | 现货 | ||
50 mg | ¥ 2,230 | 现货 | ||
100 mg | ¥ 3,730 | 现货 | ||
500 mg | ¥ 7,880 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 490 | 现货 |
产品描述 | PX-12 (PX12) (1-methylpropyl 2-imidazolyl disulfide) is a small-molecule inhibitor of Trx-1 (thioredoxin-1), stimulates apoptosis, down-regulates HIF-1α and vascular endothelial growth factor (VEGF) and inhibits tumor growth in animal models. Since high levels of Trx-1 have been associated with colorectal, gastric and lung cancers, PX-12 is indicated as a potential cancer treatment in combination with chemotherapy for patients with advanced metastatic cancer. Initial trials correlated doses of Px-12 with increased patient survival. |
靶点活性 | MCF-7 cells:1.9 μM, HT29 cells:2.9 μM |
体外活性 | In MCF-7 and HT-29 cells, PX-12 prevents the hypoxia (1% oxygen)-induced increase in HIF-1alpha protein, and decreases HIF-1-trans-activating activity, VEGF formation, and inducible nitric oxide synthase. PX-12 also inhibits the growth of MCF-7 and HT-29 cells with IC50s of 1.9 μM and 2.9 μM, respectively. [1] PX-12 also inhibits HIF-1α protein levels through an Nrf2/PMF-1-mediated increase. [2] In A549 cells, PX-12 inhibits cell growth via G2/M phase arrest, and Bax-mediated and ROS-dependent apoptosis. [3] In hepatocelluar carcinoma cells, PX-12 exerts a synergistic effect with 5-FU to significantly suppress tumorigenicity. [4] |
体内活性 | In mice bearing MCF-7 tumor xenografts, PX-12 (12 mg/kg, i.p.) decreases HIF-1α and VEGF protein levels and microvessel density. [1] |
细胞实验 | Cell growth is measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Cells are exposed to a range of concentrations of PX-12 or pleurotin for 16 h in air or hypoxia (1% oxygen). The cells are then washed with warm drug-free medium and grown in air for the remainder of the 72-h incubation.(Only for Reference) |
别名 | 2-[(1-甲基丙基)二硫代]-1H-咪唑, IV-2, PX12 |
分子量 | 188.31 |
分子式 | C7H12N2S2 |
CAS No. | 141400-58-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 38 mg/mL (201.79 mM)
DMSO: 18.8 mg/mL(100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 5.3104 mL | 26.552 mL | 53.1039 mL | 132.7598 mL |
5 mM | 1.0621 mL | 5.3104 mL | 10.6208 mL | 26.552 mL | |
10 mM | 0.531 mL | 2.6552 mL | 5.3104 mL | 13.276 mL | |
20 mM | 0.2655 mL | 1.3276 mL | 2.6552 mL | 6.638 mL | |
50 mM | 0.1062 mL | 0.531 mL | 1.0621 mL | 2.6552 mL | |
100 mM | 0.0531 mL | 0.2655 mL | 0.531 mL | 1.3276 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
PX-12 141400-58-0 Metabolism Thioredoxin IV 2 inhibit 2-[(1-甲基丙基)二硫代]-1H-咪唑 IV-2 Inhibitor IV2 PX 12 PX12 inhibitor