HJC0152-hydrochloride - STAT 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEHJC0152 hydrochlorideCat. No.: HY-100602CAS No.: 1420290-99-8分式: CHClNO分量: 406.65作靶点: STAT作通路: JAK/STAT Signaling; Stem Cell/Wnt储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 6 mg/mL (14.7

2、5 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.4591 mL 12.2956 mL 24.5912 mL5 mM 0.4918 mL 2.4591 mL 4.9182 mL10 mM 0.2459 mL 1.2296 mL 2.4591 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 HJC0152 hydrochloride信号转导和转录激活因 3 (STAT3) 的抑制剂。IC50 & Target

3、 STAT3体外研究HJC0152 hydrochloride (compound 11) significantly inhibits cell proliferation and induces apoptosisaccompanying cellular morphological changes at concentrations of 1, 5, and 10 M. Results show thattreatment with 10 M HJC0152 hydrochloride decreases the STAT3 promoter activity in MDA-MB-231

4、 cells1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEby approximately 32%, and increasing the dose of HJC0152 hydrochloride to 20 M further decreasesSTAT3 promoter activity by 62% as compare with control. Total STAT3 is reduced after treatment withHJC0152 hydrochloride. HJC0152 hydrochloride induc

5、es cleaved caspase-3 and down regulates cyclin D1 inMDA-MB-231 cells 1.体内研究 Mice treated with 7.5 mg/kg of HJC0152 hydrochloride (compound 11) via ip show a better effect in inhibitingtumor growth. The growth of xenograft tumors in mice is significantly reduced by HJC0152 hydrochloride at adose of 2

6、5 mg/kg. It is also noteworthy that HJC0152 hydrochloride does not show significant signs of toxicityat a dose of 75 mg/kg 1.PROTOCOLCell Assay 1 Breast cancer MDA-MB-231 cells are incubated in 6-well plates (2.5105/well). Cells are then treated withDMSO, or HJC0152 hydrochloride (compound 11) at di

7、fferent concentrations for 48 h, and then bothadherent and floating cells are collected, washed once with PBS. Resuspended cells are incubated with 100L PBS containing 1% BSA and 100 L Annexin V and dead cell detection reagent at room temperature for20 min. Apoptosis is measured immediately using th

8、e Muse Cell Analyzer with the MuseTM Apoptosis Kit 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Fifty-four female nude mice are are used for orthotopic tumor studies at 4 to 6 weeks of age. The mice areAdministration 1 maintained in a barrie

9、r unit with 12 h light-dark switch. Freshly harvested MDA-MB-231 cells (2.5106 cellsper mouse, resuspended in 100 L PBS) are injected into the 3rd mammary fat pad of the mice, and thenrandomly assigned into 8 groups (5 to10 mice per group). For the intraperitoneal treatment experiment, themice are t

10、reated daily with 2.5 mg/kg HJC0152 hydrochloride (compound 11) (Group A) or vehicle (Group D)when the tumor volume reaches 200 mm3. A Body weights and tumors volume are measured daily andtumor volume is calculated according to the formula V=0.5LW2, where L=length (mm) and W=width (mm)1.MCE has not

11、independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Chen H, et al. Discovery of O-Alkylamino Tethered Niclosamide Derivatives as Potent and Orally Bioavailable Anticancer Agents. ACSMed Chem Lett. 2013 Feb 14;4(2):180-185.McePdfHeightCaution: Product has not be