solo per uso di ricerca
N. Cat.S8129
| Target correlati | JAK TGF-beta/Smad ERK GSK-3 ROCK Hedgehog/Smoothened PKA Secretase STAT Casein Kinase |
|---|---|
| Altro Wnt/beta-catenin Inibitori | 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 |
| Linee cellulari | Tipo di saggio | Concentrazione | Tempo di incubazione | Formulazione | Descrizione dellattività | 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 | |
| Clicca per visualizzare più dati sperimentali sulle linee cellulari | ||||||
| Peso molecolare | 751.00 | Formula | C42H70O11 |
Conservazione (Dalla data di ricezione) | |
|---|---|---|---|---|---|
| N. CAS | 53003-10-4 | Scarica SDF | Conservazione delle soluzioni stock |
|
|
| Sinonimi | 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 | ||
|
In vitro |
DMSO
: 100 mg/mL
(133.15 mM)
Ethanol : 100 mg/mL Water : Insoluble |
|
In vivo |
|||||
Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)
Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)
Risultati del calcolo:
Concentrazione di lavoro: mg/ml;
Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.
Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.
| Targets/IC50/Ki |
Wnt/β-catenin
|
|---|---|
| In vitro |
La salinomicina, un antibiotico ionoforo polietere isolato da Streptomyces albus, ha dimostrato di uccidere le CSC in diversi tipi di tumori umani, molto probabilmente interferendo con i trasportatori di farmaci ABC (ATP-binding cassette), la via di segnalazione Wnt/β-catenina e altre vie delle CSC. Esibisce attività antimicrobica contro batteri Gram-positivi tra cui Bacillus subtilis, Staphylococcus aureus, Micrococcus flavus, Sarcina lutea, Mycobacterium spp., alcuni funghi filamentosi, Plasmodium falciparum ed Eimeria spp., parassiti protozoari responsabili della coccidiosi, una malattia del pollame. Inoltre, questo composto ha dimostrato precocemente di agire in diverse membrane biologiche, comprese le membrane citoplasmatiche e mitocondriali, come ionoforo di cationi monovalenti con stretta selettività per gli ioni alcalini e una forte preferenza per il K+, promuovendo così l'efflusso mitocondriale e citoplasmatico di K+ e inibendo la fosforilazione ossidativa. La salinomicina può indurre una massiccia apoptosi nelle cellule tumorali umane di diversa origine che mostrano molteplici meccanismi di resistenza ai farmaci e all'apoptosi.
|
| In vivo |
Salinomycin (from Streptomyces albus) è in grado di eliminare efficacemente le CSC e di indurre una regressione clinica parziale di tumori pesantemente pretrattati e resistenti alla terapia. È stato anche dimostrato come un agente inotropo e cronotropo positivo che ha aumentato la gittata cardiaca, la pressione sistolica ventricolare sinistra, la frequenza cardiaca, la pressione arteriosa media, la vasodilatazione e il flusso sanguigno delle arterie coronarie e la concentrazione di catecolamine plasmatiche. Questi risultati sono stati ottenuti in esperimenti con cani meticci che avevano ricevuto una singola iniezione endovenosa di 150 µg/kg di questo composto. Tuttavia, è stata riportata una considerevole tossicità della salinomicina nei mammiferi, come cavalli, maiali, gatti e alpaca, dopo assunzione orale o inalatoria accidentale. I dati di valutazione del rischio recentemente pubblicati dall'Autorità europea per la sicurezza alimentare dichiarano una dose giornaliera accettabile (DGA) di 5 µg/kg di salinomicina per gli esseri umani, perché l'assunzione giornaliera di più di 500 µg/kg di salinomicina da parte dei cani porta a effetti neurotossici, come perdita di mielina e degenerazione assonale. La somministrazione endovenosa di 200-250 µg/kg di salinomicina ogni due giorni per tre settimane si traduce in una regressione parziale delle metastasi tumorali e mostra solo effetti collaterali acuti e a lungo termine minori, ma nessun effetto collaterale grave acuto e a lungo termine osservato con i farmaci chemioterapici convenzionali.
|
Riferimenti |
|
Istruzioni per la manipolazione
Tel: +1-832-582-8158 Ext:3
Per qualsiasi altra domanda, si prega di lasciare un messaggio.