Bicalutamide

Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.

CAS No. 90357-06-5

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関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Exosome Secretion Related Compound Library Human Hormone Related Compound Library	もっと見る

シグナル伝達経路

Androgen Receptorシグナル伝達経路

Androgen Receptor阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
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	22672984
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	22175694
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	22391033
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	20381361
human LNCAP cells	Proliferation assay		3 days	Antiproliferative activity against human LNCAP cells after 3 days, IC50=0.7327 μM	26046313
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	24900588
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	23727044
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	SANGER
human MDA-MB-453 cells	Function assay			Displacement of [3H]R1881 from AR in human MDA-MB-453 cells, EC50=31 nM	23713567
LNCaP cells	Function assay			Inhibition of [3H]-DHT binding to T877A androgen receptor of LNCaP cells, Ki=35 nM	15603960
Freestyle293F cells	Function assay			Inhibition of wild type Androgen receptor (unknown origin) expressed in Freestyle293F cells, IC50=0.054 μM	23199477
MDA453 cells	Function assay			Displacement of [3H]DHT from human androgen receptor in MDA453 cells, Ki=64 nM	18291644
human MDA-MB-453 cells	Function assay			Displacement of [3H]DHT from AR in human MDA-MB-453 cells, IC50=64 nM	20584610
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	25646649
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	17804229
CV1 cells	Function assay			Binding affinity to human androgen receptor expressed in CV1 cells, Ki=0.151 μM	17257838
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	18442912
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	22094279
human PC3 cells	Function assay			Displacement of [3H]R1881 from androgen receptor in human PC3 cells, EC50=4.3 μM	25591066
human HT-3 cell	Growth inhibition assay			Inhibition of human HT-3 cell growth in a cell viability assay, IC50=0.73134 μM	SANGER
human CCF-STTG1 cell	Growth inhibition assay			Inhibition of human CCF-STTG1 cell growth in a cell viability assay， IC50=4.92929 μM	SANGER
human SCC-25 cell	Growth inhibition assay			Inhibition of human SCC-25 cell growth in a cell viability assay, IC50=6.08656 μM	SANGER
human MKN45 cell	Growth inhibition assay			Inhibition of human MKN45 cell growth in a cell viability assay, IC50=6.9605 μM	SANGER
human ES5 cell	Growth inhibition assay			Inhibition of human ES5 cell growth in a cell viability assay, IC50=8.61154 μM	SANGER
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	SANGER
human PC-3 cell	Growth inhibition assay			Inhibition of human PC-3 cell growth in a cell viability assay, IC50=10.2791 μM	SANGER
human NOS-1 cell	Growth inhibition assay			Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=11.2917 μM	SANGER
human LB1047-RCC cell	Growth inhibition assay			Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=12.253 μM	SANGER
human CAMA-1 cell	Growth inhibition assay			Inhibition of human CAMA-1 cell growth in a cell viability assay, IC50=12.3926 μM	SANGER
human SAS cell	Growth inhibition assay			Inhibition of human SAS cell growth in a cell viability assay, IC50=13.3081 μM	SANGER
human NCI-H2228 cell	Growth inhibition assay			Inhibition of human NCI-H2228 cell growth in a cell viability assay, IC50=13.7531 μM	SANGER
human NCI-H187 cell	Growth inhibition assay			Inhibition of human NCI-H187 cell growth in a cell viability assay, IC50=16.6616 μM	SANGER
human BFTC-905 cell	Growth inhibition assay			Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=17.4857 μM	SANGER
human G-361 cell	Growth inhibition assay			Inhibition of human G-361 cell growth in a cell viability assay, IC50=17.826 μM	SANGER
human SW780 cell	Growth inhibition assay			Inhibition of human SW780 cell growth in a cell viability assay	SANGER
human BB49-HNC cell	Growth inhibition assay			Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=18.9532 μM	SANGER
human KALS-1 cell	Growth inhibition assay			Inhibition of human KALS-1 cell growth in a cell viability assay, IC50=19.6635 μM	SANGER
human AU565 cell	Growth inhibition assay			Inhibition of human AU565 cell growth in a cell viability assay, IC50=19.7402 μM	SANGER
human NCI-H2087 cell	Growth inhibition assay			Inhibition of human NCI-H2087 cell growth in a cell viability assay, IC50=21.0591 μM	SANGER
human RVH-421 cell	Growth inhibition assay			Inhibition of human RVH-421 cell growth in a cell viability assay, IC50=21.5795 μM	SANGER
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	SANGER
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	SANGER
human NB6 cell	Growth inhibition assay			Inhibition of human NB6 cell growth in a cell viability assay, IC50=22.9135 μM	SANGER
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	SANGER
human CTB-1 cell	Growth inhibition assay			Inhibition of human CTB-1 cell growth in a cell viability assay, IC50=24.5536 μM	SANGER
human SW48 cell	Growth inhibition assay			Inhibition of human SW48 cell growth in a cell viability assay, IC50=24.6546 μM	SANGER
human TCCSUP cell	Growth inhibition assay			Inhibition of human TCCSUP cell growth in a cell viability assay, IC50=24.7232 μM	SANGER
human DK-MG cell	Growth inhibition assay			Inhibition of human DK-MG cell growth in a cell viability assay, IC50=24.8917 μM	SANGER
human ST486 cell	Growth inhibition assay			Inhibition of human ST486 cell growth in a cell viability assay, IC50=25.7464 μM	SANGER
human H4 cell	Growth inhibition assay			Inhibition of human H4 cell growth in a cell viability assay, IC50=26.9458 μM	SANGER
human SBC-1 cell	Growth inhibition assay			Inhibition of human SBC-1 cell growth in a cell viability assay, IC50=28.3507 μM	SANGER
human CAS-1 cell	Growth inhibition assay			Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=28.6294 μM	SANGER
human OAW-42 cell	Growth inhibition assay			Inhibition of human OAW-42 cell growth in a cell viability assay, IC50=28.7195 μM	SANGER
human HCC1954 cell	Growth inhibition assay			Inhibition of human HCC1954 cell growth in a cell viability assay, IC50=28.7525 μM	SANGER
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	SANGER
human MCF7 cell	Growth inhibition assay			Inhibition of human MCF7 cell growth in a cell viability assay, IC50=39.301 μM	SANGER
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生物活性

製品説明

Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.

Targets

Androgen Receptor ^[1]
(LNCaP/AR(cs) cells)

0.16 μM

In Vitro
In vitro	Bicalutamide undergoes an antagonist-to-agonist switch, stimulating AR activity. Bicalutamide 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. Bicalutamide induces cell proliferation in a dose-dependent manner, and only partially antagonized the effects of R1881. Bicalutamide treatment also results in a significant amount of nuclear AR, although less than that observed with R1881. Bicalutamide 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, Bicalutamide 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, Bicalutamide shows only weak partial antagonism of VP16-AR–mediated transcription with an IC50 of 0.35 μM. ^[1] Micromolar bicalutamide causes a significant dose-dependent reduction in clonogenicity. ^[2] Dual inhibition of the AR and mTOR signaling pathways provides further benefit with the ridaforolimus-bicalutamide combination producing syner -gistic antiproliferative effects in prostate cancer cells in vitro when compared with each agent alone. ^[3]
Kinase Assay	Whole-cell competitive binding assays
Kinase Assay	Whole-cell competitive binding assays are performed in LNCaP/AR(codon-switch) (LNCaP/AR(cs)) (harbors a mixture of exogenous wild-type AR and endogenous mutant AR (T877A)) and cells propagated in Iscove's or RPMI media supplemented with 10% fetal bovine serum, or during the assay with 10% charcoal-stripped, dextran-treated fetal bovine serum (CSS). Cells are pre-incubated with ¹⁸F-FDHT, increasing concentrations (1pM to 1μM) of cold Bicalutamide are added, and the assay is performed to measure specific uptake of ¹⁸F-FDHT (4). IC50 values are determined using a one site binding model with least squares curve fitting and R² > 0.99.
細胞実験	細胞株	C4-2 cell
	濃度	0-1 μM
	反応時間	72 hours
	実験の流れ	Exponentially growing C4-2 cells are plated into two 96-well plates and incubated overnight at 37 ˚C. Twenty-four hours later one plate is aspirated and stored at -80 ˚C and the other treated with 10-fold serial concentrations of ridaforolimus (1000 nM to 0.0001 nM) or vehicle (ethanol). Following 72 hours culture at 37 ˚C, the plates are assessed simultaneously for cell growth using the Cy qUANT Cell Proliferation Assay kit. Bicalutamide and Ridaforolimus combination proliferation assays are performed similarly except cell growth is determined as the change in cell number between vehicle control and compound treated cells after 72 hours in culture.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	Cytosolic AR / Nuclear AR		30833616
	Growth inhibition assay	Cell viability		27994514

In Vivo
In Vivo	Single bicalutamide reduces tumor growth by 79%, at defined submaximal doses. The ridaforolimus-bicalutamide 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. ^[3]
動物実験	動物モデル	Male nude mice bearing C4-2 cells
	投与量	10 mg/kg
	投与経路	Administered via p.o.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
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
NCT02146937	Withdrawn	Detectable Prostate Nodules	Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins	March 2014	Phase 2

参考
[1] Clegg NJ, et al. Cancer Res. 2012, 72(6), 1494-1503. [2] Colquhoun AJ, et al. Prostate Cancer Prostatic Dis. 2012. [3] Squillace RM, et al. Int J Oncol. 2012.

参考

化学情報

分子量	430.37	化学式	C₁₈H₁₄F₄N₂O₄S
CAS No.	90357-06-5	SDF	Download Bicalutamide SDFをダウンロードする
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
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 86 mg/mL ( (199.82 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 7 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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):