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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESalinomycinCat. No.: HY-15597CAS No.: 53003-10-4Synonyms: Procoxacin分式: CHO分量: 751作靶点: Wnt; -catenin; Bacterial; Autophagy; Mitophagy作通路: Stem Cell/Wnt; Anti-infection; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C
2、6 months-20C 1 month溶解性数据体外实验 DMSO : 36.7 mg/mL (48.87 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.3316 mL 6.6578 mL 13.3156 mL5 mM 0.2663 mL 1.3316 mL 2.6631 mL10 mM 0.1332 mL 0.6658 mL 1.3316 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。BIOLOGIC
3、AL ACTIVITY物活性 Salinomycin具有强的抗 (anti-bacterial) 活性的抗球药,和靶向类癌症细胞的新型抗癌剂。IC50 & Target IC50: 163 nM (Wnt1-stimulated reporter) 1体外研究Salinomycin is a potent inhibitor of the Wnt signaling cascade. Incubation of the malignant lymphocytes with1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESalinomycin i
4、nduces apoptosis within 48 h, with a mean IC50 of 230 nM. Salinomycin is also an antibioticpotassium ionophore, has been reported recently to act as a selective breast cancer stem cell inhibitor 1.Salinomycin is a novel and an effective anticancer drug, inhibits SW620 cells and Cisp-resistant SW620
5、cellswith IC50 of 1.540.23 M and 0.320.05 M, respectively. Salinomycin is found to have the ability to killboth cancer stem cells (CSCs) and therapy-resistant cancer cells. After continuous Salinomycin treatment for48 h, the apoptotic cells are observed under the microscope and counted randomly at l
6、east 100 cells in onefield. The number of apoptotic cells which are stained by Hoechst33342 is significantly increased in Cisp-resistant SW620 cells (20.203.72) than that of SW620 cells (9.402.07) per 100 cells (p 2.体内研究 After administration of 4 mg/kg Salinomycin (Sal), 8 mg/kg Salinomycin and 10 u
7、L/g saline water for 6 weeks,the mice are sacrificed. The size of the liver tumors in the Salinomycin treatment groups diminishes comparewith the control group. The mean diameter of the tumors decreases from 12.17 mm to 3.67 mm (p20.5) ofthe tumors decreases from 819 mm3 to 25.25 mm3 (p 3. Salinomyc
8、in is a kind of monocarboxylic acidpolyether type antibiotics, produced by the fermentation of Streptomyces albus, possesses a specific cyclicstructure, and can form a complex compound with the pathogenic microorganisms and the extracellularcations of coccidian, especially K+, Na+, Rb+, to alter the
9、 intracellular and extracellular ion concentrations4.PROTOCOLCell Assay 2 For cisplatin or Salinomycin IC50 analysis in SW620 cells or Cisp-resistant SW620 cells, cells (1104/well)are cultured in 96-well plates and treated with different chemotherapeutics (cisplatin, Salinomycin) in differentconcent
10、rations for 48 h. Then 20 L of cell counting kit-8 (CCK-8) is added into each of the 96-wells. After 4 hincubation at 37C, the optical density (OD) values are detected at 450 nm using the scan reader. Cellgrowth inhibiting rates are described as cell inhibiting curves and the IC50 parameters (inhibi
11、tingconcentration of 50% cells) are evaluated by Xlfit 5.2 software. For cell proliferation analysis, SW620 cells orCisp-resistant SW620 cells (5103/well) are also seeded in 96-well plates in serum-containing medium andtreated with cisplatin (5 M, according to the calculated IC50 values of cisplatin
12、 in SW620 cells) for 0, 12, 24,48, 72 and 96 h. Then 20 L cell counting kit-8 is added into each of the 96-wells. After 4-h incubation at37C, the coloring reactions are also quantified at 450 nm 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal M
13、ice 3Administration 34 Nude mice (nu/nu; 4-6 weeks of age) are used. HepG2 cells are suspended in 100 mL 1:1 serum-free DMEMand Matrigel. Mice are anesthetized with ketamine/xylazine and after surgically opening the abdomen,HepG2 cells are inoculated into the liver parenchyma and mice are monitored
14、every 3 days for 35 days.Finally, 18 nude mice are divided into three groups that are intraperitoneally injected daily for 6 weeks: twoSalinomycin-treated groups (4 mg/kg Salinomycin group, 8 mg/kg Salinomycin group) and the control group(saline water group).Rats 4A total of 10 male rats are used in
15、 the experiment. After a routine anesthesia, the abdomen is opened. After aresuspension of high glucose medium not containing serum DMEM, and matrigel, the bladder transitionalcancer cell line T24 is inoculated in the parenchyma of bladder in rats, and then the abdomen is sutured.2/3 Master of Small
16、 Molecules 您边的抑制剂师www.MedChemEAfter operation, the rats are randomized into the experiment group and the control group with five in eachgroup. After operation, the rats in the experiment group are immediately given intraperitoneal injection ofSalinomycin with a dosage of 8 mg/kg, while the rats in t
17、he control group are given intraperitoneal injection ofnormal saline. A close observation is paid during the drug administration period. After 15 d, the rats aresacrificed by cervical dislocation, and the complete tumor tissues are stripped to observe the tumor growthand metastasis.MCE has not indep
18、endently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Cell Commun Signal. 2018 Nov 23;16(1):89. Int J Mol Sci. 2019 Aug. Int J Mol Sci. 2019 Jun 12;20(12). pii: E2861. Oncol Rep. 2018 Aug;40(2):877-886.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Lu D, et al. Salinomycin inhibits Wnt signaling and selectively induces apoptosis in chronic lymphocytic leukemia cells. Proc Natl AcadSci U S A. 2011 Aug 9;108(32):13253-7.2. Zhou J, et al. Salinomycin induces apoptosis in cisplatin-resistan
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