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Salinomycin (Procoxacin) Wnt/beta-catenin Inhibitor

Name: Salinomycin (Procoxacin)
Brand: Selleck Chemicals
SKU: S8129
Rating: 5 (22 reviews)

Kat.-Nr.S8129

Salinomycin, traditionell als Antikokzidium eingesetzt, hat sich kürzlich als wirksam gegen Krebs und Krebsstammzellen (CSC) erwiesen.

Salinomycin (Procoxacin) Wnt/beta-catenin Inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 751.00

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Qualitätskontrolle

Charge: Reinheit: >97%

Zitiert in Nature Medicine für seine erstklassige Qualität
COA
Datenblatt
SDS

Zitiert in Nature Medicine für seine erstklassige Qualität
COA
NMR
Datenblatt
SDS

Zitiert in Nature Medicine für seine erstklassige Qualität
COA
Mikroanalyse

Warum Mikroanalyse?
Datenblatt
SDS

Verwandte Ziele	JAK TGF-beta/Smad ERK GSK-3 ROCK Hedgehog/Smoothened PKA Secretase STAT Casein Kinase
Weitere Wnt/beta-catenin Inhibitoren	IWR-1-endo PRI-724 (Foscenvivint) IWP-2 Tegatrabetan (BC-2059) Isoquercitrin ICG-001 SKL2001 BML-284 Hydrochloride (Wnt agonist 1, AMBMP) PNU-74654 FH535

Zellkultur, Behandlung & Arbeitskonzentration

Zelllinien	Assay-Typ	Konzentration	Inkubationszeit	Aktivitätsbeschreibung	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
Klicken Sie hier, um weitere experimentelle Daten zu Zelllinien anzuzeigen

Chemische Informationen, Lagerung & Stabilität

Molekulargewicht	751.00	Formel	C₄₂H₇₀O₁₁	Lagerung (Ab dem Eingangsdatum)	3 Jahre-20°CPulver
CAS-Nr.	53003-10-4	SDF herunterladen		Lagerung von Stammlösungen	1 Jahr-80°Cin Lösungsmittel 1 Monat-20°Cin Lösungsmittel
Synonyme	Procoxacin			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

Löslichkeit

In vitro
Charge:

DMSO : 100 mg/mL (133.15 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

DMSO : 100 mg/mL (133.15 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble

DMSO : 100 mg/mL (133.15 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Ethanol : 79 mg/mL

Water : Insoluble

Molaritätsrechner

Masse	Konzentration	Volumen	Molekulargewicht
=	×	×

Verdünnungsrechner Molekulargewichtsrechner

In vivo Charge:
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Von Selleck Labs validiert. Sollten Sie Anpassungen an dieser Formulierung benötigen, kontaktieren Sie unser Verkaufsteam für kundenspezifische Tests.	5.000mg/ml (6.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Von Selleck Labs validiert. Sollten Sie Anpassungen an dieser Formulierung benötigen, kontaktieren Sie unser Verkaufsteam für kundenspezifische Tests.	2.500mg/ml (3.33mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Von Selleck Labs validiert. Sollten Sie Anpassungen an dieser Formulierung benötigen, kontaktieren Sie unser Verkaufsteam für kundenspezifische Tests.	2.500mg/ml (3.33mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

Dosierung: mg/kg Durchschnittsgewicht der Tiere: g Dosiervolumen pro Tier:μL Anzahl der Tiere:

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH₂O, mischen und klären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.

Wirkmechanismus

Targets/IC₅₀/Ki	Wnt/β-catenin
In vitro	Salinomycin, ein Polyether-Ionophor-Antibiotikum, isoliert aus Streptomyces albus, hat gezeigt, dass es CSCs in verschiedenen Arten menschlicher Krebserkrankungen abtötet, höchstwahrscheinlich durch Interferenz mit ABC (ATP-binding cassette)-Arzneimitteltransportern, dem Wnt/β-Catenin-Signalweg und anderen CSC-Signalwegen. Es zeigt antimikrobielle Aktivität gegen Gram-positive Bakterien, einschließlich Bacillus subtilis, Staphylococcus aureus, Micrococcus flavus, Sarcina lutea, Mycobacterium spp., einige filamentöse Pilze, Plasmodium falciparum und Eimeria spp., Protozoenparasiten, die für die Geflügelkrankheit Kokzidiose verantwortlich sind. Darüber hinaus wurde gezeigt, dass diese Verbindung frühzeitig in verschiedenen biologischen Membranen, einschließlich zytoplasmatischer und mitochondrialer Membranen, als monovalenter Kationen-Ionophor mit strikter Selektivität für Alkalionen und einer starken Präferenz für K+ wirkt, wodurch der mitochondriale und zytoplasmatische K+-Efflux gefördert und die oxidative Phosphorylierung gehemmt wird. Salinomycin kann eine massive Apoptose in menschlichen Krebszellen unterschiedlichen Ursprungs induzieren, die multiple Mechanismen der Arzneimittel- und Apoptoseresistenz aufweisen.
In vivo	Salinomycin (from Streptomyces albus) ist in der Lage, CSCs wirksam zu eliminieren und eine teilweise klinische Regression von stark vorbehandelten und therapieresistenten Krebserkrankungen zu induzieren. Es wurde auch als positives ionotropes und chronotropes Mittel nachgewiesen, das das Herzzeitvolumen, den systolischen Druck des linken Ventrikels, die Herzfrequenz, den mittleren arteriellen Druck, die koronare Arterienvasodilatation und den Blutfluss sowie die Plasmakatecholaminkonzentration erhöhte. Diese Ergebnisse wurden in Experimenten mit Mischlingshunden erzielt, die eine einmalige intravenöse Injektion von 150 µg/kg dieser Verbindung erhalten hatten. Es wurde jedoch über eine beträchtliche Toxizität von Salinomycin bei Säugetieren wie Pferden, Schweinen, Katzen und Alpakas nach versehentlicher oraler oder inhalativer Aufnahme berichtet. Die kürzlich von der Europäischen Behörde für Lebensmittelsicherheit veröffentlichten Risikobewertungsdaten erklären eine akzeptable tägliche Aufnahmemenge (ADI) von 5 µg/kg Salinomycin für Menschen, da eine tägliche Aufnahme von mehr als 500 µg/kg Salinomycin bei Hunden zu neurotoxischen Effekten wie Myelinverlust und axonaler Degeneration führt. Die intravenöse Verabreichung von 200-250 µg/kg Salinomycin jeden zweiten Tag über drei Wochen führt zu einer teilweisen Regression von Tumormetastasen und zeigt nur geringe akute und langfristige Nebenwirkungen, jedoch keine schweren akuten und langfristigen Nebenwirkungen, die bei konventionellen chemotherapeutischen Medikamenten beobachtet werden.
Literatur	[1] https://pubmed.ncbi.nlm.nih.gov/23251084/ [2] https://pubmed.ncbi.nlm.nih.gov/23028492/ [3] https://pubmed.ncbi.nlm.nih.gov/23338561/

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