PX-12
别名: DB05448, 1-methyl propyl 2-imidazolyl disulfide
PX-12 (DB05448, 1-methyl propyl 2-imidazolyl disulfide)是一种有效的 thioredoxin-1 (Trx-1) 抑制剂，作用于 Trx-1 上 Cys73 的不可逆硫代烷基化。Phase 2。
PX-12 Chemical Structure
CAS: 141400-58-0
产品质控
批次：
纯度：
99.99%
99.99
PX-12相关产品
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细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| M21 | Function assay | 25 nM | 16 hrs | Stimulation of nuclear translocation of thioredoxin-1 from cytosol in human M21 cells at 25 nM after 16 hrs by immunocytofluorescence | 18617414 |
| Raji | Function assay | 5 to 10 uM | 4 to 24 hrs | Induction of Trx mRNA expression in human Raji cells at 5 to 10 uM after 4 to 24 hrs by RT-PCR analysis | 22128876 |
| Raji | Function assay | 10 to 20 uM | 4 to 8 hrs | Induction of Trx protein expression in human Raji cells at 10 to 20 uM after 4 to 8 hrs by Western blot analysis | 22128876 |
| T84 | Function assay | 3 hrs | Inhibition of human recombinant thioredoxin-mediated TG2 activation expressed in T84 cells assessed as blockade of 5-biotinamidopentylamine incorporation after 3 hrs by fluorescence microscopic analysis, IC50=2.11μM | 23327656 | |
| Ramos | Cytotoxicity assay | 72 hrs | Cytotoxicity against human Ramos cells after 72 hrs by MTT assay, LD50=3.4μM | 22128876 | |
| PancO2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse PancO2 cells after 72 hrs by crystal violet staining, LD50=3.9μM | 22128876 | |
| T24 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human T24 cells after 72 hrs by crystal violet staining, LD50=4.6μM | 22128876 | |
| B78 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse B78 cells after 72 hrs by crystal violet staining, LD50=5μM | 22128876 | |
| CT26 | Cytotoxicity assay | 72 hrs | Cytotoxicity against wild type mouse CT26 cells after 72 hrs by crystal violet staining, LD50=5.2μM | 22128876 | |
| K562 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human K562 cells after 72 hrs by MTT assay, LD50=5.5μM | 22128876 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by sulforhodamine B method, GI50=8.3μM | 18617414 | |
| M21 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human M21 cells after 48 hrs by sulforhodamine B method, GI50=8.3μM | 18617414 | |
| Raji | Cytotoxicity assay | 72 hrs | Cytotoxicity against human Raji cells after 72 hrs by MTT assay, LD50=8.8μM | 22128876 | |
| EMT6 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse EMT6 cells after 72 hrs by crystal violet staining, LD50=11.6μM | 22128876 | |
| HT29 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B method, GI50=25μM | 18617414 | |
| MEF | Cytotoxicity assay | Cytotoxicity against mouse MEF cells, LD50=2.7μM | 22128876 | ||
| M21 | Antiproliferative assay | Antiproliferative activity against human M21 cells, GI50=8.3μM | 18502639 | ||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells, GI50=8.3μM | 18502639 | ||
| HT29 | Antiproliferative assay | Antiproliferative activity against human HT29 cells, GI50=25μM | 18502639 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | PX-12 (DB05448, 1-methyl propyl 2-imidazolyl disulfide)是一种有效的 thioredoxin-1 (Trx-1) 抑制剂，作用于 Trx-1 上 Cys73 的不可逆硫代烷基化。Phase 2。 | |
|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | 在MCF-7和HT-29细胞中，PX-12防止低氧(1% 氧气)诱导的HIF-1alpha蛋白增加，并降低HIF-1反式激活活性，VEGF形成，和诱导型一氧化氮合酶。PX-12也会抑制MCF-7和HT-29细胞的生长，IC50s分别为1.9 μM和2.9μM。[1] PX-12也会通过Nrf2/PMF-1介导的增加抑制HIF-1α蛋白质水平。[2]在A549细胞中，PX-12通过G2/M细胞周期阻滞，和Bax-介导的，ROS-依赖性细胞凋亡抑制细胞生长。[3]在肝癌细胞中，PX-12与5-FU发挥协同作用，显著抑制致瘤性。[4] | |||
|---|---|---|---|---|
| 细胞实验 | 细胞系 | MCF-7 和 HT-29 细胞 | ||
| 浓度 | ~10 μM | |||
| 孵育时间 | 72 小时 | |||
| 方法 | 细胞生长使用3-(4,5-二甲基噻唑-2)-2,5-二苯基四氮唑溴盐法测量。在空气或低氧(1% 氧气)条件下，细胞在一系列浓度的PX-12或pleurotin中暴露16小时。然后细胞在空气中用温的不含药物的培养基洗涤，再进行后面的72小时培育。 | |||
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在负荷MCF-7肿瘤异种移植物的小鼠中，PX-12 (12 mg/kg, i.p.)降低HIF-1α 与 VEGF蛋白质水平和微血管密度。[1] | |
|---|---|---|
| 动物实验 | Animal Models | 负荷MCF-7肿瘤异种移植物的小鼠 |
| Dosages | 12 mg/kg | |
| Administration | i.p. | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00736372 | Completed | Metastatic Cancer|Advanced Cancer |
Cascadian Therapeutics Inc.|Seagen Inc. |
June 2008 | Phase 1 |
| NCT00417287 | Terminated | Pancreatic Neoplasms |
Cascadian Therapeutics Inc.|National Cancer Institute (NCI)|Translational Genomics Research Institute|Seagen Inc. |
December 2006 | Phase 2 |
化学信息&溶解度
| 分子量 | 188.31 | 分子式 | C7H12N2S2 |
| CAS号 | 141400-58-0 | SDF | Download PX-12 SDF |
| Smiles | CCC(C)SSC1=NC=CN1 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 38 mg/mL ( (201.79 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 38 mg/mL (201.79 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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