Name: Bicalutamide
Brand: Selleck Chemicals
SKU: S1190
Rating: 5 (64 reviews)

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.98%

99.98

Gerelateerde doelwitten	Adrenergic Receptor Estrogen/progestogen Receptor GPR Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor THR PGES
Overige Androgen Receptor Inhibitoren	Bavdegalutamide (ARV-110) RU58841 EPI-001 Galeterone Cyproterone Acetate 3,3'-Diindolylmethane Ailanthone JNJ-63576253 (TRC-253) Proxalutamide (GT0918) AZD3514

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving
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
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Moleculair gewicht	430.37	Formule	C₁₈H₁₄F₄N₂O₄S	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	90357-06-5	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	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

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 86 mg/mL (199.82 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	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.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Targets/IC₅₀/Ki	Androgen Receptor (LNCaP/AR(cs) cells) 0.16 μM
In vitro	Bicalutamide undergoes an antagonist-to-agonist switch, stimulating AR activity. This compound treatment of LNCaP/AR(cs) cells in absence of the synthetic androgen R1881 results in altered gene expression consistent with its well-documented agonist activity in context of AR overexpression. It induces cell proliferation in a dose-dependent manner, and only partially antagonized the effects of R1881. This chemical treatment also results in a significant amount of nuclear AR, although less than that observed with R1881. It exhibits partial agonist activity as evidenced by induction of DNA binding at AR target genes and incomplete antagonism of the effects of R1881. In absence of R1881, this agent partially activates VP16-AR–mediated transcription, indicative of AR binding to DNA. In LNCaP/AR-luc cells with a stably integrates AR-driven luciferase reporter construct. In the presence of R1881, it shows only weak partial antagonism of VP16-AR–mediated transcription with an IC50 of 0.35 μM. Micromolar bicalutamide causes a significant dose-dependent reduction in clonogenicity. Dual inhibition of the AR and mTOR signaling pathways provides further benefit with the ridaforolimus-this compound combination producing syner -gistic antiproliferative effects in prostate cancer cells in vitro when compared with each agent alone.
Kinase Assay	Whole-cell competitieve bindingsassays
Kinase Assay	Whole-cell competitieve bindingsassays worden uitgevoerd in LNCaP/AR(codon-switch) (LNCaP/AR(cs)) (bevat een mengsel van exogene wild-type AR en endogene mutante AR (T877A)) en cellen die worden gekweekt in Iscove's of RPMI-media aangevuld met 10% foetaal runderserum, of tijdens de assay met 10% met houtskool gestript, met dextran behandeld foetaal runderserum (CSS). Cellen worden voorgeïncubeerd met ¹⁸F-FDHT, toenemende concentraties (1pM tot 1μM) van koude deze verbinding worden toegevoegd, en de assay wordt uitgevoerd om de specifieke opname van ¹⁸F-FDHT (4) te meten. IC50-waarden worden bepaald met behulp van een één-plaats-bindingsmodel met curve-fitting met de kleinste kwadraten en R² > 0,99.
In vivo	Single bicalutamide reduces tumor growth by 79%, at defined submaximal doses. The ridaforolimus-this compound combination exhibits improved and potent antitumor activity, almost completely abrogating tumor growth. The combination is also well tolerated, as evidenced by no significant changes in body weight over the course of treatment. Plasma PSA levels are again tightly linked to tumor growth in the combination-treated mice.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/22266222/ [2] https://pubmed.ncbi.nlm.nih.gov/22614062/ [3] https://pubmed.ncbi.nlm.nih.gov/22614157/

Toepassingen (Applications)

Methoden	Biomarkers	Afbeeldingen	PMID
Western blot	Cytosolic AR / Nuclear AR		30833616
Growth inhibition assay	Cell viability		27994514

Informatie klinische proef (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
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

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 Antagonist

Moleculair gewicht: 430.37

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

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In vivo Formuleringscalculator (Heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Toepassingen (Applications)

Informatie klinische proef (Clinical Trial Information)

Bicalutamide Androgen Receptor Antagonist

Moleculair gewicht: 430.37

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkconcentratie (Cell Culture, Treatment & Working Concentration)

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo Formuleringscalculator (Heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Toepassingen (Applications)

Informatie klinische proef (Clinical Trial Information)

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)