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

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Controllo Qualità

Lotto: Purezza: 99.98%

99.98

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

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Descrizione dellattività
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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Informazioni chimiche, conservazione e stabilità

Peso molecolare	430.37	Formula	C₁₈H₁₄F₄N₂O₄S	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	90357-06-5	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	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

Solubilità

In vitro
Lotto:

DMSO : 86 mg/mL (199.82 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Ethanol : 7 mg/mL

Water : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

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.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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.

Meccanismo dazione

Targets/IC₅₀/Ki	Androgen Receptor (LNCaP/AR(cs) cells) 0.16 μM
In vitro	Bicalutamide subisce un interruttore da antagonista ad agonista, stimolando l'attività dell'AR. Il trattamento con questo composto di cellule LNCaP/AR(cs) in assenza dell'androgeno sintetico R1881 determina un'espressione genica alterata coerente con la sua ben documentata attività agonista nel contesto di una sovraespressione dell'AR. Induce la proliferazione cellulare in modo dose-dipendente e antagonizza solo parzialmente gli effetti di R1881. Questo trattamento chimico provoca anche una quantità significativa di AR nucleare, sebbene inferiore a quella osservata con R1881. Esibisce un'attività agonista parziale, come evidenziato dall'induzione del legame al DNA ai geni bersaglio dell'AR e dall'antagonismo incompleto degli effetti di R1881. In assenza di R1881, questo agente attiva parzialmente la trascrizione mediata da VP16-AR, indicando il legame dell'AR al DNA. Nelle cellule LNCaP/AR-luc con un costrutto reporter luciferasi guidato da AR stabilmente integrato. In presenza di R1881, mostra solo un debole antagonismo parziale della trascrizione mediata da VP16-AR con un IC50 di 0,35 μM. Il bicalutamide micromolare causa una significativa riduzione dose-dipendente della clonogenicità. La duplice inibizione delle vie di segnalazione dell'AR e di mTOR fornisce un ulteriore beneficio con la combinazione ridaforolimus-questo composto che produce effetti antiproliferativi sinergici nelle cellule di cancro alla prostata in vitro rispetto a ciascun agente da solo.
Saggio chinasico	Saggi di legame competitivo su cellule intere
Saggio chinasico	I saggi di legame competitivo su cellule intere sono eseguiti in LNCaP/AR(codon-switch) (LNCaP/AR(cs)) (che ospita una miscela di AR wild-type esogeno e AR mutante endogeno (T877A)) e cellule propagate in mezzi Iscove's o RPMI supplementati con il 10% di siero fetale bovino, o durante il saggio con il 10% di siero fetale bovino trattato con carbone e destrano (CSS). Le cellule vengono pre-incubate con ¹⁸F-FDHT, vengono aggiunte concentrazioni crescenti (da 1 pM a 1 μM) di questo composto freddo e il saggio viene eseguito per misurare l'assorbimento specifico di ¹⁸F-FDHT (4). I valori di IC50 sono determinati utilizzando un modello di legame a un sito con adattamento della curva ai minimi quadrati e R² > 0,99.
In vivo	Il solo Bicalutamide riduce la crescita tumorale del 79%, a dosi submassimali definite. La combinazione ridaforolimus-questo composto mostra un'attività antitumorale migliorata e potente, abrogando quasi completamente la crescita tumorale. La combinazione è anche ben tollerata, come evidenziato dall'assenza di cambiamenti significativi nel peso corporeo durante il corso del trattamento. I livelli plasmatici di PSA sono nuovamente strettamente collegati alla crescita tumorale nei topi trattati con la combinazione.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/22266222/ [2] https://pubmed.ncbi.nlm.nih.gov/22614062/ [3] https://pubmed.ncbi.nlm.nih.gov/22614157/

Applicazioni

Metodi	Biomarcatori	Immagini	PMID
Western blot	Cytosolic AR / Nuclear AR		30833616
Growth inhibition assay	Cell viability		27994514

Informazioni sullo studio clinico

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
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

Supporto tecnico

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

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C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Bicalutamide Androgen Receptor antagonista

Struttura chimica

Peso molecolare: 430.37