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Salinomycin (Procoxacin) Wnt/beta-catenin remmer

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

Cat.Nr.S8129

Salinomycin, traditioneel gebruikt als een anticoccidiaal medicijn, heeft recentelijk aangetoond over antikanker- en antikanker stamcel (CSC) effecten te beschikken.

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

Chemische structuur

Moleculair gewicht: 751.00

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Kwaliteitscontrole

Batch: Zuiverheid: >97%

Geciteerd in Nature Medicine voor zijn topkwaliteit
COA
Datasheet
SDS

Geciteerd in Nature Medicine voor zijn topkwaliteit
COA
NMR
Datasheet
SDS

Geciteerd in Nature Medicine voor zijn topkwaliteit
COA
Microanalyse

Waarom microanalyse?
Datasheet
SDS

Gerelateerde doelwitten	JAK TGF-beta/Smad ERK GSK-3 ROCK Hedgehog/Smoothened PKA Secretase STAT Casein Kinase
Overige 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

Celkweek, behandeling & werkconcentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	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
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht	751.00	Formule	C₄₂H₇₀O₁₁	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	53003-10-4	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	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

Oplosbaarheid

In vitro
Batch:

DMSO : 100 mg/mL (133.15 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste 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.
Clear solution	5%DMSO 1 Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste 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.
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 Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Targets/IC₅₀/Ki	Wnt/β-catenin
In vitro	Salinomycin, een polyether-ionofoor antibioticum geïsoleerd uit Streptomyces albus, heeft aangetoond CSC's te doden in verschillende typen menselijke kankers, hoogstwaarschijnlijk door interferentie met ABC (ATP-binding cassette) medicijntransporters, de Wnt/beta-catenin signaalroute en andere CSC-routes. Het vertoont antimicrobiële activiteit tegen Gram-positieve bacteriën, waaronder Bacillus subtilis, Staphylococcus aureus, Micrococcus flavus, Sarcina lutea, Mycobacterium spp., sommige filamenteuze schimmels, Plasmodium falciparum en Eimeria spp., protozoaire parasieten die verantwoordelijk zijn voor de pluimveeziekte coccidiose. Bovendien is van deze verbinding al vroeg aangetoond dat het in verschillende biologische membranen, waaronder cytoplasmatische en mitochondriale membranen, fungeert als een monovalent kationenionofoor met strikte selectiviteit voor alkalimetaalionen en een sterke voorkeur voor K+, waardoor mitochondriale en cytoplasmatische K+-uitstroom wordt bevorderd en oxidatieve fosforylering wordt geremd. Salinomycin kan massale apoptose induceren in menselijke kankercellen van verschillende oorsprong die meerdere mechanismen van medicijn- en apoptoseresistentie vertonen.
In vivo	Salinomycin (from Streptomyces albus) is in staat om CSC's effectief te elimineren en om gedeeltelijke klinische regressie te induceren van zwaar voorbehandelde en therapieresistente kankers. Het is ook aangetoond als een positief ionotropisch en chronotropisch middel dat de hartminuutvolume, de systolische druk van de linkerventrikel, de hartslag, de gemiddelde arteriële druk, coronaire vaatverwijding en bloedstroom, en de plasmacatecholamineconcentratie verhoogde. Deze resultaten zijn verkregen in experimenten met bastaardhonden die een eenmalige intraveneuze injectie van 150 μg/kg van deze verbinding hebben gekregen. Er is echter een aanzienlijke toxiciteit van Salinomycin gemeld bij zoogdieren, zoals paarden, varkens, katten en alpaca's na accidentele orale of inhalatieve inname. Risicobeoordelingsgegevens die recentelijk zijn gepubliceerd door de Europese Autoriteit voor Voedselveiligheid verklaren een aanvaardbare dagelijkse inname (ADI) van 5 μg/kg Salinomycin voor mensen, omdat dagelijkse inname van meer dan 500 μg/kg Salinomycin door honden leidt tot neurotoxische effecten, zoals myelinverlies en axonale degeneratie. Intraveneuze toediening van 200-250 μg/kg Salinomycin om de andere dag gedurende drie weken resulteert in gedeeltelijke regressie van tumormetastasen en vertoont slechts geringe acute en langetermijnbijwerkingen, maar geen ernstige acute en langetermijnbijwerkingen die worden waargenomen bij conventionele chemotherapeutische middelen.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/23251084/ [2] https://pubmed.ncbi.nlm.nih.gov/23028492/ [3] https://pubmed.ncbi.nlm.nih.gov/23338561/

Technische ondersteuning

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