1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESalinomycin sodium saltCat. No.: HY-17439CAS No.: 55721-31-8Synonyms: Salinomycin sodium; Sodium salinomycin分式: CHNaO分量: 772.98作靶點(diǎn): Bacterial作通路: Anti-infection儲(chǔ)存式: 4C, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1

2、 month (stored undernitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 15 mg/mL (19.41 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.2937 mL 6.4685 mL 12.9369 mL5 mM 0.2587 mL 1.2937 mL 2.5874 mL10 mM 0.1294 mL 0.6468 mL 1.2937 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。B

3、IOLOGICAL ACTIVITY物活性 Salinomycin sodium salt具有強(qiáng)的抗 (anti-bacterial) 活性的抗球藥，和靶向類癌癥細(xì)胞的新型抗癌劑。IC50 & Target bacterial 1體外研究Salinomycin (0.1-8 M) inhibits the growth of HUVECs in a dose-dependent manner, accounting for 32.1 and1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE59.2% inhibition at 4 and 8 M

4、, respectively. HUVECs exposed to 2, 4 and 8 M of Salinomycin for 48 hshow a dose-dependent reduction in cell number and a change in cell morphology. Salinomycin (4 M)treatment effectively inhibits HUVEC migration and invasion, and significantly disrupt the capillary-like tubeformation of HUVECs. Sa

5、linomycin significantly suppresses the expression levels of phosphorylated (p)-FAKin a time- and dose-dependent manner in HUVECs. Salinomycin inhibits HUVEC angiogenesis by disturbingthe VEGF-VEGFR2-AKT signaling axis 1. Combination of RSVL and Salinomycin synergistically inhibits theproliferation o

6、f TNBC (MDA-MB-231) cells. RSVL and Salinomycin effectively reduce wound healing, colonyand tumorosphere forming capability in TNBC cells. Synergistic combination of RSVL and Salinomycininduces apoptosis in both culture conditions by significant upregulation of Bax with decreased Bcl-2expression as

7、comparison to untreated and alone drug treatments 2. Salinomycin (0, 2, 4, 8 and 16 M)significantly inhibits the proliferation of A2780 and SK-OV-3 cell lines in a dose- and time-dependent manner,(IC50 24h: 13.8 M, IC50 48h: 6.888 M and IC50 72h: 4.382 M for A2780 cell lines), (IC50 24h: 12.7 M,IC50

8、 48h: 9.869 M and IC50 72h: 5.022 M for SK-OV-3 cell lines). Salinomycin blocks the Wnt/-cateninpathway in EOC cells 3. Salinomycin (2 M) reduces cancer cell proliferation, inhibits STAT3phosphorylation and P38 and -catenin expressions, and suppresses epithelial-mesenchymal transition incolorectal c

9、ancer cells. Salinomycin (1-5 M) inhibits cancer cell proliferation and STAT3 signaling incolorectal cancer cells. Furthermore, Salinomycin activates Akt (Ser 473) and down-regulates Hsp27 (Ser82) phosphorylation in HT-29 and SW480. Salinomycin down-regulates hTERT and reduces telomeraseactivity whe

10、n combined with telomerase inhibitor 4.體內(nèi)研究 Salinomycin (5 and 10 mg/kg) significantly supresses the average tumor volume and tumor weight.Salinomycin hinders the U251 human glioma cell growth in vivo via inhibition of angiogenesis withinvolvement of AKT and FAK dephosphorylation 1. Salinomycin (0.5

11、 mg/kg b.wt.) enhances the meansurvival time of the tumor bearing Swiss albino mice 2.PROTOCOLCell Assay 1 The effect of Salinomycin on HUVEC growth is determined by MTT assay. Briefly, HUVECs (6,000 cells/well)are seeded in 96-well culture plates for 24 h and incubated with different concentrations

12、 of Salinomycin. Inthe preliminary experiments, Salinomycin treatment for 12, 24, 48 and 72 h shows time-dependent effects oncell growth inhibition. However, treatment for 48 h is the optimal time and is selected for further mechanismevaluation. After Salinomycin treatment for 48 h, 20 L/well of MTT

13、 solution (5 mg/mL) is added andincubated for 5 h. The medium is aspirated and replaced with 200 L/well of DMSO to dissolve the formazanSalinomycint formed. The color intensity of the formazan solution is measured at 570 nm by a microplatespectrophotometer. The cell viability is expressed as % of th

14、e control (as 100%).MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Human glioma U251 cells (1107) suspended in 100 L PBS are injected into the right lower hind flank ofAdministration 1 each 6-week-old male nude mouse. The mice are then randomly

15、assigned into three groups of 10 mice ineach group. After one week, Salinomycin (5 and 10 mg/kg) is administered into the caudal vein every otherday for 16 days. Control mice receive an equal volume of vehicle (Salinomycinine) only. Body weight andtumor volume are monitored every two days. At the en

16、d of the experiments, tumors are excised,photographed, and weighed. Tumors from each group are used for western blotting and2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEimmunohistochemical (IHC) assay.MCE has not independently confirmed the accuracy of these methods. They are for reference only.

17、戶使本產(chǎn)品發(fā)表的科研獻(xiàn) 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. Bi YL, et al. Salinomycin exhibits anti-angiogenic activity against hu

18、man glioma in vitro and in vivo by suppressing the VEGF-VEGFR2-AKT/FAK signaling axis. Int J Mol Med. 2017 Mar 292. Rai G, et al. Evaluation of growth inhibitory response of Resveratrol and Salinomycin combinations against triple negative breast cancercells. Biomed Pharmacother. 2017 Mar 11;89:1142-11513. Li R, et al. Salinomycin repressed the epithelial-mesenchymal transition of epithelial ovarian cancer cells via downregulating Wnt/-catenin pathway. Onco Targets Ther. 2017 Feb 28;10:1317-1324. Chung SS, et al. Salinomycin Abolished STAT3 and STAT1 Interactions and Reduced