Salinomycin (from Streptomyces albus)

Synonyms: Procoxacin

Salinomycin, traditionally used as an anti-coccidial drug, has recently been shown to possess anti-cancer and anti-cancer stem cell (CSC) effects.

Salinomycin (from Streptomyces albus) Chemical Structure

Salinomycin (from Streptomyces albus) Chemical Structure

CAS No. 53003-10-4

Purity & Quality Control

Salinomycin (from Streptomyces albus) Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HL60 cells Proliferation assay 72 h Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.29 μM 25644674
MV4-11 cells Proliferation assay 72 h Antiproliferative activity against human MV4-11 cells after 72 hrs, IC50=0.33 μM 26163197
LoVo cells Proliferation assay 72 h Antiproliferative activity against human LoVo cells assessed as growth inhibition after 72 hrs by SRB method, IC50=0.36 μM 25644674
VCaP cells Proliferation assay Antiproliferative activity against human VCaP cells, EC50=0.38 μM 23063400
LS180 cells Proliferation assay 72 h Antiproliferative activity against human LS180 cells assessed as growth inhibition after 72 hrs by SRB method, IC50=0.61 μM 25644674
HT-29 cells Proliferation assay 72 h Antiproliferative activity against human HT-29 cells assessed as growth inhibition after 72 hrs by SRB method, IC50=1.03 μM 25644674
SW707 cells Proliferation assay 72 h Antiproliferative activity against human SW707 cells assessed as growth inhibition after 72 hrs by SRB method, IC50=1.73 μM 25644674
HL60/Vinc cells Cytotoxicity assay 72 h Cytotoxicity against vincristine-resistant human HL60/Vinc cells incubated for 72 hrs by MTT assay, IC50=3.44 μM 23079523
BALB/3T3 cells Cytotoxicity assay 72 h Cytotoxicity against mouse BALB/3T3 cells incubated for 72 hrs by MTT assay, IC50=28.08 μM 23079523
VCaP Antiproliferative assay Antiproliferative activity against human VCaP cells, EC50 = 0.38 μM. 23063400
HL60 Cytotoxicity assay 72 hrs Cytotoxicity against human HL60 cells incubated for 72 hrs by MTT assay, IC50 = 0.44 μM. 23079523
LoVo Cytotoxicity assay 72 hrs Cytotoxicity against human LoVo cells incubated for 72 hrs by MTT assay, IC50 = 1.11 μM. 23079523
HL60/Vinc Cytotoxicity assay 72 hrs Cytotoxicity against vincristine-resistant human HL60/Vinc cells incubated for 72 hrs by MTT assay, IC50 = 3.44 μM. 23079523
LoVo/DX Cytotoxicity assay 72 hrs Cytotoxicity against doxorubicin-resistant human LoVo/DX cells incubated for 72 hrs by MTT assay, IC50 = 6.23 μM. 23079523
BALB/3T3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BALB/3T3 cells incubated for 72 hrs by MTT assay, IC50 = 28.08 μM. 23079523
LoVo/DX Antiproliferative assay Antiproliferative activity against human LoVo/DX cells, IC50 = 1 μM. 24631190
HL60 Antiproliferative assay Antiproliferative activity against human HL60 cells, IC50 = 1.2 μM. 24631190
LoVo Antiproliferative assay Antiproliferative activity against human LoVo cells, IC50 = 1.5 μM. 24631190
HL60/Vinc Antiproliferative assay Antiproliferative activity against human HL60/Vinc cells, IC50 = 4.7 μM. 24631190
BALB/3T3 Antiproliferative assay Antiproliferative activity mouse BALB/3T3 cells, IC50 = 25.8 μM. 24631190
HL60 Antiproliferative assay 72 hrs Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.29 μM. 25644674
LoVo Antiproliferative assay 72 hrs Antiproliferative activity against human LoVo cells assessed as growth inhibition after 72 hrs by SRB method, IC50 = 0.36 μM. 25644674
LS180 Antiproliferative assay 72 hrs Antiproliferative activity against human LS180 cells assessed as growth inhibition after 72 hrs by SRB method, IC50 = 0.61 μM. 25644674
LoVo/DX Antiproliferative assay 72 hrs Antiproliferative activity against human doxorubicin-resistant LoVo/DX cells assessed as growth inhibition after 72 hrs by SRB method, IC50 = 0.76 μM. 25644674
HT-29 Antiproliferative assay 72 hrs Antiproliferative activity against human HT-29 cells assessed as growth inhibition after 72 hrs by SRB method, IC50 = 1.03 μM. 25644674
SW707 Antiproliferative assay 72 hrs Antiproliferative activity against human SW707 cells assessed as growth inhibition after 72 hrs by SRB method, IC50 = 1.73 μM. 25644674
HL60/Vinc Antiproliferative assay 72 hrs Antiproliferative activity against human vincristine-resistant HL60/Vinc cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 2.09 μM. 25644674
BALB/3T3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BALB/3T3 cells assessed as growth inhibition after 72 hrs by SRB method, IC50 = 9.33 μM. 25644674
MV4-11 Antiproliferative assay 72 hrs Antiproliferative activity against human MV4-11 cells after 72 hrs, IC50 = 0.33 μM. 26163197
LoVo Antiproliferative assay 72 hrs Antiproliferative activity against human LoVo cells after 72 hrs, IC50 = 0.53 μM. 26163197
LoVo/DX Antiproliferative assay 72 hrs Antiproliferative activity against doxorubicin-resistant human LoVo/DX cells after 72 hrs, IC50 = 0.59 μM. 26163197
BALB/3T3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BALB/3T3 cells after 72 hrs, IC50 = 27.76 μM. 26163197
JIMT1 Cytotoxicity assay 72 hrs Cytotoxicity against human JIMT1 cells after 72 hrs by MTT assay, IC50 = 0.52 μM. 27326340
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 0.59 μM. 27326340
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 2.98 μM. 27876192
MDA-MB-231 Antiproliferative assay 48 hrs Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 6.42 μM. 27876192
MIAPaCa2 Cytotoxicity assay 48 hrs Cytotoxicity against human MIAPaCa2 cells assessed as decrease in cell viability after 48 hrs by MTS assay 28177244
DU145 Cytotoxicity assay 48 hrs Cytotoxicity against human DU145 cells assessed as decrease in cell viability after 48 hrs by MTS assay 28177244
BT474 Cytotoxicity assay 48 hrs Cytotoxicity against human BT474 cells assessed as decrease in cell viability after 48 hrs by MTS assay 28177244
MDA-MB-231 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell viability after 48 hrs by MTS assay 28177244
HT-29 Cytotoxicity assay 48 hrs Cytotoxicity against human HT-29 cells assessed as decrease in cell proliferation after 48 hrs by MTT assay, IC50 = 1.43 μM. 28262526
HGC27 Cytotoxicity assay 48 hrs Cytotoxicity against human HGC27 cells assessed as decrease in cell proliferation after 48 hrs by MTT assay, IC50 = 2.57 μM. 28262526
MDA-MB-231 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell proliferation after 48 hrs by MTT assay, IC50 = 6.53 μM. 28262526
OV2008 Cytotoxicity assay 72 hrs Cytotoxicity against human OV2008 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 3.2 μM. 28651817
OV2008 Cytotoxicity assay 48 hrs Cytotoxicity against human OV2008 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay, IC50 = 4.78 μM. 28651817
OV2008 Cytotoxicity assay 24 hrs Cytotoxicity against human OV2008 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay, IC50 = 7.44 μM. 28651817
HT-29 Antiproliferative assay 48 hrs Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay, IC50 = 1.43 μM. 28688275
HEK293 Cytotoxicity assay 72 hrs Cytotoxicity against HEK293 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.195 μM. 29466777
HEK293 Cytotoxicity assay 72 hrs Cytotoxicity against doxycycline inducible T-Rex/K-Ras G12V HEK293 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.3295 μM. 29466777
HL60 Cytotoxicity assay 48 hrs Cytotoxicity against human HL60 cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 0.58 μM. 29466777
SW480 Cytotoxicity assay 48 hrs Cytotoxicity against human SW480 cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 3.77 μM. 29466777
4T1 Cytotoxicity assay 48 hrs Cytotoxicity against mouse 4T1 cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 3.78 μM. 29466777
A549 Cytotoxicity assay 48 hrs Cytotoxicity against human A549 cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 3.98 μM. 29466777
HeLa Cytotoxicity assay 48 hrs Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 4.49 μM. 29466777
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 9.08 μM. 29466777
SMMC7721 Cytotoxicity assay 48 hrs Cytotoxicity against human SMMC7721 cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 12.04 μM. 29466777
BEAS2B Cytotoxicity assay 48 hrs Cytotoxicity against human BEAS2B cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 13.07 μM. 29466777
LoVo Antiproliferative assay 72 hrs Antiproliferative activity against human LoVo cells after 72 hrs by SRB assay, IC50 = 0.44 μM. 30025346
LoVo/DX Antiproliferative assay 72 hrs Antiproliferative activity against human LoVo/DX cells after 72 hrs by SRB assay, IC50 = 0.69 μM. 30025346
SK-BR-3 Antiproliferative assay 72 hrs Antiproliferative activity against human SK-BR-3 cells after 72 hrs by SRB assay, IC50 = 0.89 μM. 30025346
JIMT1 Antiproliferative assay 72 hrs Antiproliferative activity against human JIMT1 cells after 72 hrs by SRB assay, IC50 = 1.3 μM. 30025346
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay, IC50 = 1.5 μM. 30025346
ALL5 Antiproliferative assay 120 hrs Antiproliferative activity against human ALL5 cells after 120 hrs by MTT assay, IC50 = 2.4 μM. 30025346
MCF10A Antiproliferative assay 72 hrs Antiproliferative activity against human MCF10A cells after 72 hrs by SRB assay, IC50 = 46 μM. 30025346
HMLER Antiproliferative assay Antiproliferative activity against HMLER cells by MTT assay Breast cancer stem cell, IC50 = 0.1 μM. 30684870
HeLa Antiproliferative assay Antiproliferative activity against human HeLa cells by MTT assay, IC50 = 0.32 μM. 30684870
LoVo Antiproliferative assay Antiproliferative activity against human LoVo cells by SRB assay, IC50 = 0.44 μM. 30684870
JIMT1 Antiproliferative assay Antiproliferative activity against human JIMT1 cells, IC50 = 0.52 μM. 30684870
JIMT1 Antiproliferative assay Antiproliferative activity against human JIMT1 cells by MTT assay, IC50 = 0.52 μM. 30684870
MCF7 Antiproliferative assay Antiproliferative activity against human MCF7 cells by MTT assay, IC50 = 0.59 μM. 30684870
LoVo/DX Antiproliferative assay Antiproliferative activity against human LoVo/DX cells by SRB assay, IC50 = 0.69 μM. 30684870
SKBR3 Antiproliferative assay Antiproliferative activity against human SKBR3 cells by SRB assay, IC50 = 0.89 μM. 30684870
HT-29 Antiproliferative assay Antiproliferative activity against human HT-29 cells by MTT assay, IC50 = 1.03 μM. 30684870
JIMT1 Antiproliferative assay Antiproliferative activity against human JIMT1 cells by SRB assay, IC50 = 1.3 μM. 30684870
MCF7 Antiproliferative assay Antiproliferative activity against human MCF7 cells by SRB assay, IC50 = 1.5 μM. 30684870
HGC27 Antiproliferative assay Antiproliferative activity against human HGC27 cells by MTT assay, IC50 = 2.57 μM. 30684870
HT-29 Antiproliferative assay 48 hrs Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay, IC50 = 3.21 μM. 30684870
4T1 Antiproliferative assay Antiproliferative activity against mouse 4T1 cells by MTT assay, IC50 = 3.78 μM. 30684870
A549 Antiproliferative assay Antiproliferative activity against human A549 cells by MTT assay, IC50 = 3.98 μM. 30684870
MDA-MB-231 Antiproliferative assay Antiproliferative activity against human MDA-MB-231 cells by SRB assay, IC50 = 6.42 μM. 30684870
MDA-MB-231 Antiproliferative assay Antiproliferative activity against human MDA-MB-231 cells by MTT assay, IC50 = 6.91 μM. 30684870
HGC27 Antiproliferative assay 48 hrs Antiproliferative activity against human HGC27 cells after 48 hrs by MTT assay, IC50 = 8.18 μM. 30684870
Caco2 Antiproliferative assay Antiproliferative activity against human Caco2 cells by MTT assay, IC50 = 12.99 μM. 30684870
U87 Antiproliferative assay Antiproliferative activity against human U87 cells by MTT assay, IC50 = 38.7 μM. 30684870
MCF10A Antiproliferative assay Antiproliferative activity against human MCF10A cells by SRB assay, IC50 = 46 μM. 30684870
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 24.5 μM. 30871771
HL60 Cytotoxicity assay 24 hrs Cytotoxicity against human HL60 cells assessed as growth inhibition after 24 hrs by resazurin dye based assay, GI50 = 6.63 μM. 30986574
HL-60 Function assay 24 hrs Trypanocidal activity against bloodstream forms of Trypanosoma brucei infected in human HL-60 cells incubated for 24 hrs followed by compound wash out after 72 hrs, GI50 = 0.18 μM. 31103901
MDCK Antiviral assay 3 days Antiviral activity against Influenza A virus (A/Hong Kong/7/1987(H3N2)) infected in MDCK cells after 3 days by MTT assay, EC50 = 0.4 μM. 31103901
Vero Antiviral assay 24 hrs Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr, IC50 = 0.24 μM. ChEMBL
MIAPaCa2 Cytotoxicity assay 48 hrs Cytotoxicity against human MIAPaCa2 cells after 48 hrs by MTS assay, CC50 = 6.5 μM. ChEMBL
BT474 Cytotoxicity assay 48 hrs Cytotoxicity against human BT474 cells after 48 hrs by MTS assay, CC50 = 14 μM. ChEMBL
BT474 Function assay 7.5 uM 3 days Disruption of preformed spheroids in human BT474 cancer stem cells at 7.5 uM after 3 days by microscopic analysis ChEMBL
DU145 Function assay 7.5 uM 3 days Disruption of preformed spheroids in human DU145 cancer stem cells at 7.5 uM after 3 days by microscopic analysis ChEMBL
Click to View More Cell Line Experimental Data

Biological Activity

Description Salinomycin, traditionally used as an anti-coccidial drug, has recently been shown to possess anti-cancer and anti-cancer stem cell (CSC) effects.
Targets
Wnt/β-catenin [1]
In vitro
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].
Cell Research Cell lines colon cancer (SW480, SW620, RKO) and breast cancer cell lines (MCF-7, T47D, MDA-MB-453).
Concentrations 1, 2.5, 5, 10 μM
Incubation Time 26 h
Method

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.

In Vivo
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].
Animal Research Animal Models NOD/SCID mice
Dosages 5 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 751.00 Formula

C42H70O11

CAS No. 53003-10-4 SDF Download Salinomycin (from Streptomyces albus) SDF
Smiles CCC(C1CCC(C(O1)C(C)C(C(C)C(=O)C(CC)C2C(CC(C3(O2)C=CC(C4(O3)CCC(O4)(C)C5CCC(C(O5)C)(CC)O)O)C)C)O)C)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (133.15 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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