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CAS No.: 141400-58-0

PX-12 Catalog No. CSN13688

Synonyms: IV-2

PX-12 is an irreversible thioredoxin-1 (Trx-1) inhibitor with antitumor activity.

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生物活性

实验方案

技术信息

生物活性

描述The high expression of redox protein thioredoxin-1 (Trx-1) has been reported in many human cancers, which increases the resistance of cells to apoptosis and induces the production of angiogenic factors. PX-12 is a potent inhibitor of Trx-1. It inhibits the growth of HT-29 and MCF-7 cells with IC50 values of 2.9  2.0μM and 1.9  0.8μM, respectively. The exposure of MCF-7 cells with PX-12 during hypoxia dose-dependently reduced the protein expression of hypoxia-inducible factor-1 (HIF-1) with an IC50 of 7.2  0.9μM. PX-12 also resulted in significant inhibition of hypoxia-induced HIF-1 trans-activating activity in MCF-7 cells with an IC50 of 11.5 ± 1.1μM. The hypoxia-stimulated formation of vascular endothelial growth factor (VEGF) was decreased by PX-12 treatment in both MCF-7 and HT-29 cells with IC50 values of 10.4 ± 2.5 and 10.1 ± 2.2μM, respectively. In mice with MCF-7 tumor xenografts, i.p. administration of 12mg/kg PX-12 significantly decreased VEGF protein expression and microvessel density 24 hours after the injection as compared with untreated animals^[3]. PX-12 at 0.1-100μM inhibits the thioredoxin system mediated gp120 reduction in a concentration dependent manner, thus showing anti-HIV-1 activity in TZM-bl cells^[4].
作用机制PX-12 potently inhibits Trx-1 via the irreversible thioalkylation of the Cys73 residue, leading to the inhibition of Trx-dependent cell growth^[3].
动物研究
剂量
Mice: 30 mg/kg^[3] (i.p.); 25 mg/kg^[4] (i.v.)

给药途径
i.p., i.v.
临床研究

动物研究
剂量	Mice: 30 mg/kg^[3] (i.p.); 25 mg/kg^[4] (i.v.)
给药途径	i.p., i.v.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00736372	Metastatic Cancer ... more >> Advanced Cancer Collapse <<	Phase 1	Completed	-	United States, Arizona ... more >> TGen Clinical Research Services at Scottsdale Healthcare Scottsdale, Arizona, United States, 85258 United States, South Carolina Cancer Centers of the Carolinas Greenville, South Carolina, United States, 29605 United States, Texas Tyler Cancer Center Tyler, Texas, United States, 75702 Collapse <<
NCT00417287	Pancreatic Neoplasms	Phase 2	Terminated(Investigator decisi... more >>on) Collapse <<	-	United States, Arizona ... more >> TGen Clinical Research Services at Scottsdale Healthcare Scottsdale, Arizona, United States, 85258 Arizona Cancer Center, University of Arizona Tucson, Arizona, United States, 85724 United States, Texas The University of Texas M.D. Anderson Cancer Center Houston, Texas, United States, 77030 Collapse <<

参考文献

[1] Kim YH, Coon A, et al. Antitumor agent PX-12 inhibits HIF-1α protein levels through an Nrf2/PMF-1-mediated increase in spermidine/spermine acetyl transferase. Cancer Chemother Pharmacol. 2011 Aug;68(2):405-13.
[2] Welsh SJ, Williams RR, 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.
[3] Welsh SJ, Williams RR, Birmingham A, Newman DJ, Kirkpatrick DL, Powis G. 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.
[4] Lundberg M, Mattsson Å, Reiser K, Holmgren A, Curbo S. Inhibition of the thioredoxin system by PX-12 (1-methylpropyl 2-imidazolyl disulfide) impedes HIV-1 infection in TZM-bl cells. Sci Rep. 2019 Apr 4;9(1):5656.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 5.3103 mL
- 26.5515 mL
- 53.1029 mL
- 5 mM
- 1.0621 mL
- 5.3103 mL
- 10.6206 mL
- 10 mM
- 0.5310 mL
- 2.6551 mL
- 5.3103 mL

技术信息

CAS号

141400-58-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C7H12N2S2

运输

蓝冰

分子量

188.31

别名

IV-2

溶解度

DMSO	18.83 mg/mL (100.0 mM)
Water	N/A

动物实验配方

2% DMSO+30% PEG 300+water

11 mg/mL

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