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Purity: ≥98%
Salinomycin (also known as AHR-3096, or Procoxacin) is a potent antibacterial and coccidiostat ionophore therapeutic agent with potential anticancer activities by targeting stem cells. Salinomycin (Procoxacin) has been shown by Piyush Gupta to kill breast cancer stem cells at least 100 times more effectively than another popular anti-cancer compound (paclitaxel) in mice. The mechanism of action by which salinomycin (Procoxacin) kills cancer stem cells specifically remains unknown, but is thought to be due to its action as a potassium ionophore due to the detection of Nigericin in the same compound screen. Salinomycin has high toxicity and a narrow therapeutic window which may limit its clinical use.
| ln Vitro |
Salinomycin is a strong Wnt signaling cascade agent. With an average IC50 of 230 nM, salinomycin oxazoline can be produced in cells in 48 hours. Another antibacterial potassium ionophore is salinomycin. According to recent reports, it is a novel and potent anti-cancer medication for breast cancer stem cells. The SW620 cells and Cisp-resistant SW620 cells are inhibited by salinomycin, with IC50 values of 1.54±0.23 μM and 0.32±0.05 μM, respectively. It was discovered that salinomycin had the ability to destroy cancer stem cells (CSC) and their carrying capacity. Following a 48-hour period of continuous salinomycin treatment, the stained cells were examined under a microscope, and a minimum of 100 cells were randomly counted within each field of view. The amount of Hoechst33342-stained cells in Cisp-resistant SW620 cells (20.20±3.72) revealed a significant difference from 9.40±2.07)/100 cells in SW620 cells (p<0.05). Both Cisp-resistant and SW620 cells were found using flow cytometric analysis 48 hours after the cells were treated with salinomycin. Compared to SW620 cells (16.78±2.56%), the disinfection rate of Cisp (37.82±3.63%) was much greater (p<0.05).[2].
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| ln Vivo |
After receiving 4 mg/kg of salinomycin (Sal), 8 mg/kg of salinomycin, and 10 μL/g of saline, the mice were sacrificed six weeks later. When compared to the control group, the liver tumor size was smaller in the salinomycin-treated group. There was a significant drop in the average tumor diameter (from 12.17 mm to 3.67 mm; p<0.05) and average tumor volume (V=length×width2×0.5) from 819 mm3 to 25.25 mm3. To assess salinomycin's antitumor activity, tumors were then removed and put through immunohistochemistry, TUNEL assay, and HE staining. The tissue structure of liver cancer is revealed by HE staining, which displays nuclei of varying sizes as well as the destroyed liver cord structure. Following salinomycin treatment, immunohistochemistry revealed decreased PCNA expression. The cell apoptosis rate was higher in the salinomycin-treated group than in the control group, as demonstrated by HE staining and the TUNEL assay. Moreover, immunohistochemistry demonstrated that the treatment with salinomycin increased the Bax/Bcl-2 ratio. The group treated with salinomycin had lower levels of β-catenin protein expression than the control group [4]. Streptomyces albicans fermentation results in the production of salinomycin, a monocarboxylic acid polyether antibiotic. Its unique ring structure enables it to form complexes with the extracellular cations of coccidia and pathogenic microorganisms, particularly K+, Na+, and Rb+, which alters the ion concentration both inside and outside of the cell [5].
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| References |
[1]. Lu D, et al. Salinomycin inhibits Wnt signaling and selectively induces apoptosis in chronic lymphocytic leukemia cells. Proc Natl Acad Sci U S A. 2011 Aug 9;108(32):13253-7.
[2]. Zhou J, et al. Salinomycin induces apoptosis in cisplatin-resistant colorectal cancer cells by accumulation of reactiveoxygen species. Toxicol Lett. 2013 Oct 24;222(2):139-45. [3]. Klose J, et al. Salinomycin: Anti-tumor activity in a pre-clinical colorectal cancer model. PLoS One. 2019 Feb 14;14(2):e0211916. [4]. Wang F, et al. Salinomycin Inhibits Proliferation and Induces Apoptosis of Human Hepatocellular Carcinoma Cells In Vitro and In Vivo. PLoS One. 2012; 7(12): e50638. [5]. Qu H, et al. Effect of salinomycin on metastasis and invasion of bladder cancer cell line T24. Asian Pac J Trop Med. 2015 Jul;8(7):578-82. [6]. Naujokat C, et al. Salinomycin as a drug for targeting human cancer stem cells. J Biomed Biotechnol. 2012;2012:950658 |
| Molecular Formula |
C42H70O11
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| Molecular Weight |
751.00
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| CAS # |
53003-10-4
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| Related CAS # |
Salinomycin sodium salt;55721-31-8
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| SMILES |
[H][C@]1([C@](C)(CC2)O[C@]32[ C@H](O)C=C[C@]4(O[C@]([H])([C@@H](CC)C([C@@H](C)[C@@H](O)[ C@H](C)[C@]5([H])O[C@]([C@@H](CC)C(O)=O)([H])CC[C@@H]5C)=O)[C@@H](C)C[ C@H]4C)O3)CC [C@@](CC)(O)[ C@H](C)O1
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3316 mL | 6.6578 mL | 13.3156 mL | |
| 5 mM | 0.2663 mL | 1.3316 mL | 2.6631 mL | |
| 10 mM | 0.1332 mL | 0.6658 mL | 1.3316 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Sal inhibits HCC cell proliferationin vitro.PLoS One.2012;7(12):e50638. |
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 Sal causes cell cycle arrest and induces apoptosis of HCC cellsin vitro.PLoS One.2012;7(12):e50638. |
 Sal increases intracellular Calcium levelsin vitro.PLoS One.2012;7(12):e50638. |
 Anti-tumor activity of Salin vivo.A. HE staining showed the structure of the liver cancer tissue: nuclei of different sizes, hepatic cord structure was destroyed. B. Immunohistochemistry indicates that PCNA expression is down-regulated after Sal.PLoS One.2012;7(12):e50638. |
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 A. Gross observation of HepG2 cell orthotopic tumors in nude mice from the saline group or Sal groups (4 mg/kg or 8 mg/kg). B. Tendency of tumor mean diameter after injection in nude mice (*p<0.05).PLoS One.2012;7(12):e50638. |
 A. Real-time PCR was performed to examine mRNA expression of the Wnt pathway.PLoS One.2012;7(12):e50638. |
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