pour la recherche uniquement
Réf. CatalogueS8129
| Cibles apparentées | JAK TGF-beta/Smad ERK GSK-3 ROCK Hedgehog/Smoothened PKA Secretase STAT Casein Kinase |
|---|---|
| Autre Wnt/beta-catenin Inhibiteurs | 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 |
| 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 | |
| Cliquez pour voir plus de données expérimentales sur la lignée cellulaire | ||||||
| Poids moléculaire | 751.00 | Formule | C42H70O11 |
Stockage (À compter de la date de réception) | |
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| N° CAS | 53003-10-4 | Télécharger le SDF | Stockage des solutions mères |
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| 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 | ||
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In vitro |
DMSO
: 100 mg/mL
(133.15 mM)
Ethanol : 100 mg/mL Water : Insoluble |
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In vivo |
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Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)
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.)
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.
| Targets/IC50/Ki |
Wnt/β-catenin
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|---|---|
| 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.
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| 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.
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Références |
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