solo para uso en investigación

Salinomycin (Procoxacin) Wnt/beta-catenin inhibidor

Cat. No.S8129

La Salinomycin, tradicionalmente utilizada como fármaco anticoccidial, ha demostrado recientemente poseer efectos anticancerígenos y contra las células madre cancerosas (CSC).
Salinomycin (Procoxacin) Wnt/beta-catenin inhibidor Chemical Structure

Estructura química

Peso molecular: 751.00

Saltar a

Control de calidad

Lote: Pureza: >97%
97

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares Tipo de ensayo Concentración Tiempo de incubación Formulación Descripción de la actividad 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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Información química, almacenamiento y estabilidad

Peso molecular 751.00 Fórmula

C42H70O11

Almacenamiento (Desde la fecha de recepción)
Nº CAS 53003-10-4 Descargar SDF Almacenamiento de soluciones madre

Sinónimos 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

Solubilidad

In vitro
Lote:

DMSO : 100 mg/mL (133.15 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 100 mg/mL

Water : Insoluble

Calculadora de Molaridad

Masa Concentración Volumen Peso molecular
Calculadora de Dilución Calculadora de Peso Molecular

In vivo
Lote:

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

mg/kg g μL

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH2O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción

Targets/IC50/Ki
Wnt/β-catenin
In vitro
La salinomicina, un antibiótico ionóforo de poliéter aislado de Streptomyces albus, ha demostrado eliminar las CSC en diferentes tipos de cánceres humanos, muy probablemente interfiriendo con los transportadores de fármacos ABC (cassette de unión a ATP), la vía de señalización Wnt/β-catenina y otras vías de CSC. Exhibe actividad antimicrobiana contra bacterias Grampositivas, incluyendo Bacillus subtilis, Staphylococcus aureus, Micrococcus flavus, Sarcina lutea, Mycobacterium spp., algunos hongos filamentosos, Plasmodium falciparum y Eimeria spp., parásitos protozoarios responsables de la coccidiosis, una enfermedad aviar. Además, se ha demostrado que este compuesto actúa tempranamente en diferentes membranas biológicas, incluidas las membranas citoplasmáticas y mitocondriales, como un ionóforo de cationes monovalentes con estricta selectividad para los iones alcalinos y una fuerte preferencia por el K+, promoviendo así el eflujo mitocondrial y citoplasmático de K+ e inhibiendo la fosforilación oxidativa. La salinomicina puede inducir apoptosis masiva en células cancerosas humanas de diferente origen que presentan múltiples mecanismos de resistencia a fármacos y apoptosis.
In vivo
Salinomycin (from Streptomyces albus) es capaz de eliminar eficazmente las CSC e inducir una regresión clínica parcial de cánceres fuertemente pretratados y resistentes a la terapia. También se ha demostrado como un agente inotrópico y cronotrópico positivo que aumentó el gasto cardíaco, la presión sistólica ventricular izquierda, la frecuencia cardíaca, la presión arterial media, la vasodilatación y el flujo sanguíneo de las arterias coronarias y la concentración plasmática de catecolaminas. Estos resultados se obtuvieron en experimentos con perros mestizos que habían recibido una única inyección intravenosa de 150 µg/kg de este compuesto. Sin embargo, se ha informado de una toxicidad considerable de salinomicina en mamíferos, como caballos, cerdos, gatos y alpacas, después de una ingesta oral o inhalatoria accidental. Los datos de evaluación de riesgos publicados recientemente por la Autoridad Europea de Seguridad Alimentaria declaran una ingesta diaria aceptable (IDA) de 5 µg/kg de salinomicina para humanos, ya que la ingesta diaria de más de 500 µg/kg de salinomicina por perros conduce a efectos neurotóxicos, como pérdida de mielina y degeneración axonal. La administración intravenosa de 200-250 µg/kg de salinomicina cada dos días durante tres semanas da como resultado una regresión parcial de la metástasis tumoral y muestra solo efectos secundarios agudos y a largo plazo menores, pero no se observaron efectos secundarios agudos y a largo plazo graves con los fármacos quimioterapéuticos convencionales.
Referencias

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