Name: Bicalutamide
Brand: Selleck Chemicals
SKU: S1190
Rating: 5 (63 reviews)

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Control de calidad

Lote: Pureza: 99.98%

99.98

Dianas relacionadas	Adrenergic Receptor Estrogen/progestogen Receptor GPR Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor PGES THR
Otros Androgen Receptor Inhibidores	Bavdegalutamide (ARV-110) RU58841 EPI-001 Galeterone Cyproterone Acetate 3,3'-Diindolylmethane Ailanthone Proxalutamide (GT0918) AZD3514 Chlormadinone acetate

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Descripción de la actividad
human MDA-MB-453 cells	Function assay			Displacement of [3H]R1881 from AR in human MDA-MB-453 cells, EC50=31 nM
LNCaP cells	Function assay			Inhibition of [3H]-DHT binding to T877A androgen receptor of LNCaP cells, Ki=35 nM
Freestyle293F cells	Function assay			Inhibition of wild type Androgen receptor (unknown origin) expressed in Freestyle293F cells, IC50=0.054 μM
HEK293 cells	Function assay		3 h	Displacement of [17-alpha-methyl-3H]mibolerone from androgen receptor expressed in HEK293 cells after 3 hrs, IC50=54 nM
MDA453 cells	Function assay			Displacement of [3H]DHT from human androgen receptor in MDA453 cells, Ki=64 nM
human MDA-MB-453 cells	Function assay			Displacement of [3H]DHT from AR in human MDA-MB-453 cells, IC50=64 nM
COS1 cells	Function assay			Antagonist activity against pSG5-tagged human androgen receptor expressed in COS1 cells assessed as reduction in receptor-mediated transcriptional activity by AR-regulated rat probasin promoter fragment driven firefly luciferase reporter assay, IC50=0.0869 μM
HeLa cells	Function assay			Antagonist activity at human androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone induced transcriptional activity by reporter gene assay, IC50=0.14 μM
CV1 cells	Function assay			Binding affinity to human androgen receptor expressed in CV1 cells, Ki=0.151 μM
monkey COS7 cells	Function assay			Binding affinity to human androgen receptor expressed in monkey COS7 cells by whole cell binding assay, Ki=0.151 μM
COS7 cells	Function assay			Agonist activity at human androgen receptor W741C mutant expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay, EC50=0.18 μM
CHO-K1 cells	Function assay		2 h	Displacement of [3H]mibolerone from human AR expressed in CHO-K1 cells after 2 hrs by scintillation counting, IC50=0.2 μM
human HT-3 cell	Growth inhibition assay			Inhibition of human HT-3 cell growth in a cell viability assay, IC50=0.73134 μM
human LNCAP cells	Proliferation assay		3 days	Antiproliferative activity against human LNCAP cells after 3 days, IC50=0.7327 μM
human PC3 cells	Function assay			Displacement of [3H]R1881 from androgen receptor in human PC3 cells, EC50=4.3 μM
human 22Rv1 cells	Function assay		3 days	Antagonist activity at androgen receptor H874Y mutant (unknown origin) expressed in human 22Rv1 cells assessed as inhibition of DHT-induced cell growth after 3 days by WST-8 assay, IC50=4.6 μM
human CCF-STTG1 cell	Growth inhibition assay			Inhibition of human CCF-STTG1 cell growth in a cell viability assay， IC50=4.92929 μM
human SCC-25 cell	Growth inhibition assay			Inhibition of human SCC-25 cell growth in a cell viability assay, IC50=6.08656 μM
human MKN45 cell	Growth inhibition assay			Inhibition of human MKN45 cell growth in a cell viability assay, IC50=6.9605 μM
human ES5 cell	Growth inhibition assay			Inhibition of human ES5 cell growth in a cell viability assay, IC50=8.61154 μM
human SK-MEL-3 cell	Growth inhibition assay			Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=10.0964 μM
human PC-3 cell	Growth inhibition assay			Inhibition of human PC-3 cell growth in a cell viability assay, IC50=10.2791 μM
human NOS-1 cell	Growth inhibition assay			Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=11.2917 μM
human LB1047-RCC cell	Growth inhibition assay			Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=12.253 μM
human CAMA-1 cell	Growth inhibition assay			Inhibition of human CAMA-1 cell growth in a cell viability assay, IC50=12.3926 μM
human SAS cell	Growth inhibition assay			Inhibition of human SAS cell growth in a cell viability assay, IC50=13.3081 μM
human NCI-H2228 cell	Growth inhibition assay			Inhibition of human NCI-H2228 cell growth in a cell viability assay, IC50=13.7531 μM
human NCI-H187 cell	Growth inhibition assay			Inhibition of human NCI-H187 cell growth in a cell viability assay, IC50=16.6616 μM
human BFTC-905 cell	Growth inhibition assay			Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=17.4857 μM
human G-361 cell	Growth inhibition assay			Inhibition of human G-361 cell growth in a cell viability assay, IC50=17.826 μM
human DU145 cells	Cytotoxic assay		72 h	Cytotoxicity against ERalpha-deficient human DU145 cells expressing ERbeta assessed as growth inhibition after 72 hrs by MTT assay, IC50=18 μM
human SW780 cell	Growth inhibition assay			Inhibition of human SW780 cell growth in a cell viability assay
human BB49-HNC cell	Growth inhibition assay			Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=18.9532 μM
human KALS-1 cell	Growth inhibition assay			Inhibition of human KALS-1 cell growth in a cell viability assay, IC50=19.6635 μM
human AU565 cell	Growth inhibition assay			Inhibition of human AU565 cell growth in a cell viability assay, IC50=19.7402 μM
human NCI-H2087 cell	Growth inhibition assay			Inhibition of human NCI-H2087 cell growth in a cell viability assay, IC50=21.0591 μM
human RVH-421 cell	Growth inhibition assay			Inhibition of human RVH-421 cell growth in a cell viability assay, IC50=21.5795 μM
human SK-CO-1 cell	Growth inhibition assay			Inhibition of human SK-CO-1 cell growth in a cell viability assay, IC50=21.8872 μM
human KU-19-19 cell	Growth inhibition assay			Inhibition of human KU-19-19 cell growth in a cell viability assay, IC50=22.0242 μM
human NB6 cell	Growth inhibition assay			Inhibition of human NB6 cell growth in a cell viability assay, IC50=22.9135 μM
human RO82-W-1 cell	Growth inhibition assay			Inhibition of human RO82-W-1 cell growth in a cell viability assay, IC50=23.1318 μM
human LNCAP cells	Cytotoxic assay		2 days	Cytotoxicity against human LNCAP cells assessed as cell viability after 2 days by cell counting method, IC50=23.79 μM
human CTB-1 cell	Growth inhibition assay			Inhibition of human CTB-1 cell growth in a cell viability assay, IC50=24.5536 μM
human SW48 cell	Growth inhibition assay			Inhibition of human SW48 cell growth in a cell viability assay, IC50=24.6546 μM
human TCCSUP cell	Growth inhibition assay			Inhibition of human TCCSUP cell growth in a cell viability assay, IC50=24.7232 μM
human DK-MG cell	Growth inhibition assay			Inhibition of human DK-MG cell growth in a cell viability assay, IC50=24.8917 μM
human ST486 cell	Growth inhibition assay			Inhibition of human ST486 cell growth in a cell viability assay, IC50=25.7464 μM
human H4 cell	Growth inhibition assay			Inhibition of human H4 cell growth in a cell viability assay, IC50=26.9458 μM
human SBC-1 cell	Growth inhibition assay			Inhibition of human SBC-1 cell growth in a cell viability assay, IC50=28.3507 μM
human CAS-1 cell	Growth inhibition assay			Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=28.6294 μM
human OAW-42 cell	Growth inhibition assay			Inhibition of human OAW-42 cell growth in a cell viability assay, IC50=28.7195 μM
human HCC1954 cell	Growth inhibition assay			Inhibition of human HCC1954 cell growth in a cell viability assay, IC50=28.7525 μM
human MDA-MB-453 cell	Growth inhibition assay			Inhibition of human MDA-MB-453 cell growth in a cell viability assay, IC50=29.907 μM
human MCF7 cell	Growth inhibition assay			Inhibition of human MCF7 cell growth in a cell viability assay, IC50=39.301 μM
human PC3 cells	Function assay	100　μM	48 h	Inhibition of actin based pseudopodia formation in androgen-dependent human PC3 cells at 100 uM after 48 hrs by DAPI staining based fluorescence microscopy assay
human PC3 cells	Function assay	0.1-1 μM		Agonist activity at androgen receptor W741C mutant expressed in human PC3 cells assessed as stimulation of receptor transactivation at 0.1 to 1 uM by luciferase reporter gene assay
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Información química, almacenamiento y estabilidad

Peso molecular	430.37	Fórmula	C₁₈H₁₄F₄N₂O₄S	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	90357-06-5	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	ICI-176334			Smiles	CC(CS(=O)(=O)C1=CC=C(C=C1)F)(C(=O)NC2=CC(=C(C=C2)C#N)C(F)(F)F)O

Solubilidad

In vitro
Lote:

DMSO : 86 mg/mL (199.82 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 7 mg/mL

Water : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	4.350mg/ml (10.11mM)	Taking the 1 mL working solution as an example, add 50 μL of 87 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 95% Corn oil Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	4.350mg/ml (10.11mM)	Taking the 1 mL working solution as an example, add 50 μL of 87 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.
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.
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.

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)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

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	Androgen Receptor (LNCaP/AR(cs) cells) 0.16 μM
In vitro	Bicalutamide experimenta un cambio de antagonista a agonista, estimulando la actividad del AR. El tratamiento de células LNCaP/AR(cs) con este compuesto en ausencia del andrógeno sintético R1881 resulta en una expresión génica alterada consistente con su actividad agonista bien documentada en el contexto de la sobreexpresión de AR. Induce la proliferación celular de manera dosis-dependiente y solo antagoniza parcialmente los efectos de R1881. Este tratamiento químico también resulta en una cantidad significativa de AR nuclear, aunque menor que la observada con R1881. Exhibe actividad agonista parcial como lo demuestra la inducción de la unión al ADN en genes diana del AR y el antagonismo incompleto de los efectos de R1881. En ausencia de R1881, este agente activa parcialmente la transcripción mediada por VP16-AR, lo que indica la unión del AR al ADN. En células LNCaP/AR-luc con un constructo reportero de luciferasa impulsado por AR integrado de forma estable. En presencia de R1881, muestra solo un débil antagonismo parcial de la transcripción mediada por VP16-AR con una IC50 de 0,35 μM. Bicalutamida micromolar causa una reducción significativa dosis-dependiente en la clonogenicidad. La doble inhibición de las vías de señalización de AR y mTOR proporciona un beneficio adicional con la combinación ridaforolimus-este compuesto que produce efectos antiproliferativos sinérgicos en células de cáncer de próstata in vitro en comparación con cada agente solo.
Ensayo de quinasa	Ensayos de unión competitiva en células completas
Ensayo de quinasa	Los ensayos de unión competitiva en células enteras se realizan en LNCaP/AR(cambio de codón) (LNCaP/AR(cs)) (que alberga una mezcla de AR exógeno de tipo salvaje y AR mutante endógeno (T877A)) y células propagadas en medios Iscove's o RPMI suplementados con 10% de suero fetal bovino, o durante el ensayo con 10% de suero fetal bovino tratado con carbón activado y dextrano (CSS). Las células se preincuban con ¹⁸F-FDHT, se añaden concentraciones crecientes (1 pM a 1 μM) de este compuesto frío, y el ensayo se realiza para medir la captación específica de ¹⁸F-FDHT (4). Los valores de IC50 se determinan utilizando un modelo de unión de un sitio con ajuste de curva por mínimos cuadrados y R² > 0,99.
In vivo	El Bicalutamide solo reduce el crecimiento tumoral en un 79%, a dosis submaximales definidas. La combinación ridaforolimus-este compuesto exhibe una actividad antitumoral mejorada y potente, abrogando casi por completo el crecimiento tumoral. La combinación también es bien tolerada, como lo demuestra la ausencia de cambios significativos en el peso corporal durante el curso del tratamiento. Los niveles plasmáticos de PSA están nuevamente estrechamente vinculados al crecimiento tumoral en los ratones tratados con la combinación.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/22266222/ [2] https://pubmed.ncbi.nlm.nih.gov/22614062/ [3] https://pubmed.ncbi.nlm.nih.gov/22614157/

Aplicaciones

Métodos	Biomarcadores	Imágenes	PMID
Western blot	Cytosolic AR / Nuclear AR		30833616
Growth inhibition assay	Cell viability		27994514

Información del ensayo clínico

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
NCT06222593	Not yet recruiting	Carcinoma Renal Cell	State University of New York at Buffalo	June 1 2024	Phase 1\|Phase 2
NCT04573231	Recruiting	Breast Cancer\|HER2-negative Breast Cancer\|Metastatic Breast Cancer	University of Wisconsin Madison	May 24 2021	Phase 2
NCT04443062	Recruiting	Prostate Cancer	Radboud University Medical Center\|Prostaatkankerstichting\|Advanced Accelerator Applications	July 20 2020	Phase 2
NCT02910050	Unknown status	Breast Cancer	Xu fei\|Sun Yat-sen University	January 2016	Phase 2

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Instrucciones de manipulación

Tel: +1-832-582-8158 Ext:3

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Bicalutamide Androgen Receptor antagonista

Estructura química

Peso molecular: 430.37