Salinomycin (from Streptomyces albus)

製品コードS8129 バッチS812901

印刷

化学情報

 Chemical Structure Synonyms Procoxacin Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C42H70O11

分子量 751.00 CAS No. 53003-10-4
Solubility (25°C)* 体外 DMSO 100 mg/mL (133.15 mM)
Ethanol 79 mg/mL (105.19 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Salinomycin (Procoxacin), traditionally used as an anti-coccidial drug, has recently been shown to possess anti-cancer and anti-cancer stem cell (CSC) effects.
in vitro Salinomycin, a polyether ionophore antibiotic isolated from Streptomyces albus, has been shown to kill CSCs in different types of human cancers, most likely by interfering with ABC(ATP-binding cassette) drug transporters, the Wnt/β-catenin signaling pathway, and other CSC pathways. Salinomycin exhibits antimicrobial activity against Gram-positive bacteria including Bacillus subtilis, Staphylococcus aureus, Micrococcus flavus, Sarcina lutea, Mycobacterium spp., some filamentous fungi, Plasmodium falciparum, and Eimeria spp., protozoan parasites responsible for the poultry disease coccidiosis. In addition, salinomycin has early been shown to act in different biological membranes, including cytoplasmic and mitochondrial membranes, as a monovalent cation ionophore with strict selectivity for alkali ions and a strong preference for K+, thereby promoting mitochondrial and cytoplasmic K+ efflux and inhibiting oxidative phosphorylation. Salinomycin can induce massive apoptosis in human cancer cells of different origin that display multiple mechanisms of drug and apoptosis resistance[1].
in vivo Salinomycin is able to effectively eliminate CSCs and to induce partial clinical regression of heavily pretreated and therapy-resistant cancers. It has also been demonstrated as a positive ionotropic and chronotropic agent that increased cardiac output, left ventricular systolic pressure, heart rate, mean arterial pressure, coronary artery vasodilatation and blood flow, and plasma catecholamine concentration. These results have been obtained in experiments with mongrel dogs that has received a single intravenous injection of 150 μg/kg salinomycin. However, It has been reported with a considerable toxicity of salinomycin in mammals, such as horses, pigs, cats, and alpacas after accidental oral or inhalative intake. Risk assessment data recently published by the European Food Safety Authority declare an acceptable daily intake (ADI) of 5 μg/kg salinomycin for humans, because daily intake of more than 500 μg/kg salinomycin by dogs leads to neurotoxic effects, such as myelin loss and axonal degeneration. Intravenous administration of 200-250 μg/kg salinomycin every second day for three weeks results in partial regression of tumor metastasis and shows only minor acute and long-term side effects, but no severe acute and long-term side effects observed with conventional chemotherapeutic drugs[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 colon cancer (SW480, SW620, RKO) and breast cancer cell lines (MCF-7, T47D, MDA-MB-453).
濃度 1, 2.5, 5, 10 μM
反応時間 26 h
実験の流れ

Cells are plated at 1500 (SW480 or SW620) or 4000 (all other cell lines) per well in flat-bottom 96-well plates. They are treated with salinomycin at the indicated concentration 16 hours later. Seventy-two hours after this, 5 mg/ml MTT in PBS is added per well; cells are lysed after 4 hours by addition of 50 µl triplex solution (10% SDS; 5% isobutanol, 0.012 M HCl). Absorbance is measured at 562 nm. Alternatively, viability is determined with the ViaCount reagent on a Guava easyCyte8HT flow cytometer, following the instructions of the manufacturer.

動物実験 動物モデル NOD/SCID mice
投薬量 5 mg/kg
投与方法 i.p.

カスタマーフィードバック

Data from [Data independently produced by , , Tumour Biol, 2016, 305-11]

Data from [Data independently produced by , , Tumor and Stem Cell Biology, 2015, 75(21):4582-4592.]

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

MUC1-C is a target of salinomycin in inducing ferroptosis of cancer stem cells [ Cell Death Discov, 2024, 10(1):9] PubMed: 38182558
Using a Quantitative High-Throughput Screening Platform to Identify Molecular Targets and Compounds as Repurposing Candidates for Endometriosis [ Biomolecules, 2023, 13(6)965] PubMed: 37371546
Inhibiting BRAF/EGFR/MEK suppresses cancer stemness and drug resistance of primary colorectal cancer cells [ Oncotarget, 2023, 14:879-889] PubMed: 37791907
Inhibiting BRAF/EGFR/MEK suppresses cancer stemness and drug resistance of primary colorectal cancer cells [ Oncotarget, 2023, 10.18632/oncotarget.28517] PubMed: 37791907
WNT Co-Receptor LRP6 Is Critical for Zygotic Genome Activation and Embryonic Developmental Potential by Interacting with Oviductal Paracrine Ligand WNT2 [ Genes (Basel), 2023, 14(4)891] PubMed: 37107647
Curcumin Analog, HO-3867, Induces Both Apoptosis and Ferroptosis via Multiple Mechanisms in NSCLC Cells with Wild-Type p53 [ Evid Based Complement Alternat Med, 2023, 2023:8378581] PubMed: 36814470
Salinomycin-Loaded High-Density Lipoprotein Exerts Promising Anti-Ovarian Cancer Effects by Inhibiting Epithelial-Mesenchymal Transition [ Int J Nanomedicine, 2022, 17:4059-4071] PubMed: 36105618
Avasimibe Alleviates Disruption of the Airway Epithelial Barrier by Suppressing the Wnt/β-Catenin Signaling Pathway [ Front Pharmacol, 2022, 13:795934] PubMed: 35222024
In Vitro Antiviral Activities of Salinomycin on Porcine Epidemic Diarrhea Virus [ Viruses, 2021, 13(4)580] PubMed: 33808275
Inhibition of Wnt/β-catenin Pathway Reverses Multi-Drug Resistance and EMT in Oct4 +/Nanog + NSCLC Cells [ Biomed Pharmacother, 2020, 16;127:110225] PubMed: 32428834

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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