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Salinomycin sodium (also known as Procoxacin, AHR-3096) is a potent antibacterial and coccidiostat ionophore therapeutic agent with potential anticancer activities by targeting stem cells. Piyush Gupta has demonstrated in mice that salinomycin (Procoxacin) kills breast cancer stem cells at least 100 times more effectively than another well-known anti-cancer drug, paclitaxel. Salinomycin (Procoxacin) is thought to act as a potassium ionophore due to the discovery of Nigericin in the same compound screen, though the exact mechanism by which it kills cancer stem cells is still unknown. Salinomycin's clinical use may be constrained by its high level of toxicity and constrained therapeutic window.
| Targets |
Wnt/β-catenin
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|---|---|
| ln Vitro |
Salinomycin sodium salt (2, 4 and 8 μM) and salinomycin sodium salt (0.1-8 μM; 48 h) decreased HUVEC growth by 32.1% and 59.2%, respectively. 48 h) of HUVEC exhibited a dose-dependent reduction in cell quantity and shape. Salinomycin (4 μM) reduced HUVEC migration and damaged their capillary-like tube formation. Salinomycin dramatically reduced the expression of phosphorylated (p)-FAK in HUVECs in a time and dose-dependent manner. Salinomycin suppresses HUVEC angiogenesis by disrupting the VEGF-VEGFR2-AKT signaling pathway [1]. RSVL and Salinomycin work synergistically to suppress TNBC (MDA-MB-231) cells. RSVL and salinomycin have been shown to efficiently decrease TNBC cells' wound healing, colony and tumor sphere forming abilities. The effective combination of RSVL and salinomycin generated cytokines by dramatically increasing Bax and lowering Bcl-2 expression in both culture conditions when compared to untreated and medication treatment alone [2]. Salinomycin (0, 2, 4, 8, and 16 μM) dramatically reduced motility in A2780 and SK-OV-3 cell lines in a dose- and time-dependent manner. The IC50 values for the A2780 cell line are 13.8 μM at 24 hours, 6.888 μM at 48 hours, and 4.382 μM at 72 hours. For the SK-OV-3 cell line, they are 12.7 μM at 24 hours, 9.869 μM at 48 hours, and 5.022 μM at 72 hours. Salinomycin prevents Wnt/β-catenin staining in EOC cells [3]. Salinomycin (2 μM) inhibits STAT3 phosphorylation, suppresses P38 and β-catenin production, and promotes epithelial-mesenchymal transition in the rectal tract. Salinomycin (1-5 μM) reduces ischemia and STAT3 signaling in the rectal tract. In addition, salinomycin stimulates Akt (Ser 473) and monitors Hsp27 (Ser 82) phosphorylation in HT-29 and SW480. Salinomycin, in conjunction with telomerase reduction, folds hTERT and decreases telomerase activity [4].
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| ln Vivo |
The mean tumor volume and tumor weight were considerably decreased by salinomycin (5 and 10 mg/kg). Salinomycin inhibits angiogenesis and involves itself in the dephosphorylation of AKT and FAK, which prevents the growth of U251 human neurotumor cells in vivo [1]. Swiss albino mice with tumors can sleep longer on average when given salinomycin (0.5 mg/kg) [2].
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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 |
| Molecular Formula |
C₄₂H₆₉NAO₁₁
|
|---|---|
| Molecular Weight |
772.98
|
| Exact Mass |
772.47375729
|
| CAS # |
55721-31-8
|
| Related CAS # |
Salinomycin;53003-10-4
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| Appearance |
Solid
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| SMILES |
CC[C@H]([C@H]1CC[C@@H]([C@@H](O1)[C@@H](C)[C@@H]([C@H](C)C(=O)[C@H](CC)[C@@H]2[C@H](C[C@H]([C@]3(O2)C=C[C@H]([C@@]4(O3)CC[C@@](O4)(C)[C@H]5CC[C@@]([C@@H](O5)C)(CC)O)O)C)C)O)C)C(=O)[O-].[Na+]
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| InChi Key |
YPZYGIQXBGHDBH-UZHRAPRISA-M
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| InChi Code |
InChI=1S/C42H70O11.Na/c1-11-29(38(46)47)31-15-14-23(4)36(50-31)27(8)34(44)26(7)35(45)30(12-2)37-24(5)22-25(6)41(51-37)19-16-32(43)42(53-41)21-20-39(10,52-42)33-17-18-40(48,13-3)28(9)49-33;/h16,19,23-34,36-37,43-44,48H,11-15,17-18,20-22H2,1-10H3,(H,46,47);/q;+1/p-1/t23-,24-,25+,26-,27-,28-,29+,30-,31+,32+,33+,34+,36+,37-,39-,40+,41-,42-;/m0./s1
|
| Chemical Name |
sodium;(2R)-2-[(2R,5S,6R)-6-[(2S,3S,4S,6R)-6-[(3S,5S,7R,9S,10S,12R,15R)-3-[(2R,5R,6S)-5-ethyl-5-hydroxy-6-methyloxan-2-yl]-15-hydroxy-3,10,12-trimethyl-4,6,8-trioxadispiro[4.1.57.35]pentadec-13-en-9-yl]-3-hydroxy-4-methyl-5-oxooctan-2-yl]-5-methyloxan-2-yl]butanoate
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| Synonyms |
Salinomycin sodium; Procoxacin
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO: ~100 mg/mL (~129.4 mM)
H2O: <0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2937 mL | 6.4685 mL | 12.9369 mL | |
| 5 mM | 0.2587 mL | 1.2937 mL | 2.5874 mL | |
| 10 mM | 0.1294 mL | 0.6468 mL | 1.2937 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.
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