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Salinomycin (Procoxacin) Wnt/beta-catenin inhibiteur

Réf. CatalogueS8129

Le Salinomycin, traditionnellement utilisé comme anticoccidien, s'est récemment avéré posséder des effets anticancéreux et anti-cellules souches cancéreuses (CSC).
Salinomycin (Procoxacin) Wnt/beta-catenin inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 751.00

Aller à

Contrôle qualité

Lot : Pureté: >97%
97

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires Type dessai Concentration Temps dincubation Formulation Description de lactivité 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
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Informations chimiques, stockage et stabilité

Poids moléculaire 751.00 Formule

C42H70O11

Stockage (À compter de la date de réception)
N° CAS 53003-10-4 Télécharger le SDF Stockage des solutions mères

Synonymes 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

Solubilité

In vitro
Lot:

DMSO : 100 mg/mL (133.15 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Ethanol : 100 mg/mL

Water : Insoluble

Calculateur de molarité

Masse Concentration Volume Poids moléculaire
Calculateur de dilution Calculateur de poids moléculaire

In vivo
Lot:

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

mg/kg g μL

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH2O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.

Note : 1. Veuillez vous assurer que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue, lors de lajout précédent, est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Targets/IC50/Ki
Wnt/β-catenin
In vitro
Le Salinomycin, un antibiotique ionophore polyéther isolé de Streptomyces albus, a été montré pour tuer les CSC dans différents types de cancers humains, très probablement en interférant avec les transporteurs de médicaments ABC (ATP-binding cassette), la voie de signalisation Wnt/beta-catenin et d'autres voies de CSC. Il présente une activité antimicrobienne contre les bactéries Gram-positives, y compris Bacillus subtilis, Staphylococcus aureus, Micrococcus flavus, Sarcina lutea, Mycobacterium spp., certains champignons filamenteux, Plasmodium falciparum et Eimeria spp., parasites protozoaires responsables de la coccidiose chez la volaille. De plus, ce composé a été montré très tôt pour agir dans différentes membranes biologiques, y compris les membranes cytoplasmiques et mitochondriales, comme un ionophore de cations monovalents avec une sélectivité stricte pour les ions alcalins et une forte préférence pour le K+, favorisant ainsi l'efflux mitochondrial et cytoplasmique de K+ et inhibant la phosphorylation oxydative. Le Salinomycin peut induire une apoptose massive dans les cellules cancéreuses humaines d'origines différentes qui présentent de multiples mécanismes de résistance aux médicaments et à l'apoptose.
In vivo
Salinomycin (from Streptomyces albus) est capable d'éliminer efficacement les CSC et d'induire une régression clinique partielle des cancers lourdement prétraités et résistants à la thérapie. Il a également été démontré comme un agent inotrope et chronotrope positif qui a augmenté le débit cardiaque, la pression systolique ventriculaire gauche, la fréquence cardiaque, la pression artérielle moyenne, la vasodilatation et le flux sanguin des artères coronaires, et la concentration plasmatique de catécholamines. Ces résultats ont été obtenus lors d'expériences avec des chiens bâtards ayant reçu une seule injection intraveineuse de 150 µg/kg de ce composé. Cependant, une toxicité considérable du salinomycin a été rapportée chez les mammifères, tels que les chevaux, les porcs, les chats et les alpagas après une ingestion orale ou inhalative accidentelle. Les données d'évaluation des risques récemment publiées par l'Autorité européenne de sécurité des aliments déclarent une dose journalière admissible (DJA) de 5 µg/kg de salinomycin pour les humains, car une prise quotidienne de plus de 500 µg/kg de salinomycin par les chiens entraîne des effets neurotoxiques, tels que la perte de myéline et la dégénérescence axonale. L'administration intraveineuse de 200 à 250 µg/kg de salinomycin tous les deux jours pendant trois semaines entraîne une régression partielle des métastases tumorales et ne montre que des effets secondaires aigus et à long terme mineurs, mais aucun effet secondaire grave aigu et à long terme observé avec les médicaments chimiothérapeutiques conventionnels.
Références

Support technique

Instructions de manipulation

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