Bicalutamide

别名: ICI-176334 中文名称：比卡鲁胺

目录号：S1190 Purity: 99.96%

Bicalutamide是一种androgen receptor (AR)拮抗剂，在LNCaP/AR(cs)细胞系中IC50为0.16 μM。Bicalutamide 可诱导自噬。

Bicalutamide Chemical Structure

CAS: 90357-06-5

规格	价格	库存
10mM (1mL in DMSO)	1470	现货
50mg	988.18	现货
200mg	3014.55	现货
1g	7944.3	现货
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产品质控

批次：纯度： 99.96%

99.96

Bicalutamide相关产品

相关产品	Galeterone EPI-001 Cyproterone Acetate 3,3'-Diindolylmethane Bavdegalutamide (ARV-110)	点击展开
相关化合物库	FDA药物库天然产物库已知活性药物库-I 外泌体分泌相关化合物库人类激素相关化合物库	点击展开

细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述
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
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
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 LNCAP cells	Proliferation assay		3 days	Antiproliferative activity against human LNCAP cells after 3 days, IC50=0.7327 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 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 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 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
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
human PC3 cells	Function assay			Displacement of [3H]R1881 from androgen receptor in human PC3 cells, EC50=4.3 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 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 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 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
点击查看更多细胞系数据

生物活性

产品描述

Bicalutamide是一种androgen receptor (AR)拮抗剂，在LNCaP/AR(cs)细胞系中IC50为0.16 μM。Bicalutamide 可诱导自噬。

特性

Bicalutamide 和Enzalutamide联用治疗前列腺肿瘤已经进入二期临床实验阶段。

靶点

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

0.16 μM

体外研究(In Vitro)
体外研究活性	Bicalutamide 经过一个拮抗剂到激活剂的转变，刺激AR活性。在缺乏合成雄激素R1881的情况下，Bicalutamide处理LNCaP/AR(cs)细胞，改变基因表达，与其记录的良好激活剂活性相符合。Bicalutamide诱导细胞增殖，这种作用存在剂量依赖性，且只部分抗R1881的效果。Bicalutamide 处理呀显著产生大量核AR,虽然比R1881处理的少。Bicalutamide通过诱导DNA在AR靶基因结合，而具有部分激活剂活性，且不完全抗 R1881的效果。在R1881存在时, Bicalutamide部分激活 VP16-AR调节的转录，指导AR 结合到DNA上。使用AR驱动的荧光素酶报告结构稳定整合到LNCaP/AR-luc细胞中。在R1881存在时, Bicalutamide只微弱且部分抗 VP16-AR调节的转录，IC50 为 0.35 μM。^[1] 微摩尔 Bicalutamide显著降低集落形成，这种作用存在剂量依赖性。^[2] 双重抑制 AR 和 mTOR信号通路产生进一步好处，在体外，Ridaforolimus-Bicalutamide联用作用于前列腺癌细胞，与单独药剂处理相比，产生协同抗增殖效果。^[3]
细胞实验	细胞系	C4-2细胞系
	浓度	0 nM-1 μM
	孵育时间	72小时
	方法	指数生长的C4-2细胞接种到96孔板中，在37^oC下温育过夜。24小时后，吸除其中一个板，然后储存在-80^oC中，其他使用10倍系列浓度 Ridaforolimus(1000 nM 到0.0001 nM)或乙醇（对照）处理。在 37^oC下培养72小时，使用Cy qUANT细胞增殖检测试剂盒测评细胞生长。
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	Cytosolic AR / Nuclear AR		30833616
	Growth inhibition assay	Cell viability		27994514

体内研究(In Vivo)
体内研究活性	Bicalutamide按规定的次最大剂量单独处理，降低79%肿瘤生长。Ridaforolimus-Bicalutamide 联用具有改进的和有效的抗肿瘤活性，几乎完全废除肿瘤生长。联合使用具有良好耐受性，在处理过程中体重没有明显改变。联用处理的小鼠中，血浆PSA水平与肿瘤生长紧密相关。^[3]
动物实验	Animal Models	携带C4-2细胞的雄性裸鼠
	Dosages	10 mg/kg
	Administration	口服处理

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

参考文献
https://pubmed.ncbi.nlm.nih.gov/22266222/ https://pubmed.ncbi.nlm.nih.gov/22614062/ https://pubmed.ncbi.nlm.nih.gov/22614157/

参考文献

https://pubmed.ncbi.nlm.nih.gov/22266222/
https://pubmed.ncbi.nlm.nih.gov/22614062/
https://pubmed.ncbi.nlm.nih.gov/22614157/

化学信息&溶解度

分子量	430.37	分子式	C₁₈H₁₄F₄N₂O₄S
CAS号	90357-06-5	SDF	Download Bicalutamide SDF
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
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 86 mg/mL ( (199.82 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 5 mg/mL (11.61 mM)

Water : Insoluble

DMSO : 86 mg/mL ( (199.82 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 4 mg/mL (9.29 mM)

Water : Insoluble

DMSO : 86 mg/mL ( (199.82 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 5 mg/mL (11.61 mM)

Water : Insoluble

DMSO : 87 mg/mL ( (202.15 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 7 mg/mL (16.26 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解配方批次：现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂				动物体内配方计算器
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	4.350mg/ml (10.11mM)	以 1 mL 工作液为例,取50μL87mg/ml的澄清DMSO储备液加到400μLPEG300中,混合均匀使其澄清;向上述体系中加入50μLTween80,混合均匀使其澄清;然后继续加入500μLddH2O定容至1mL。工作液请现配现用!
澄清溶液	5% DMSO 1 95% Corn oil 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	4.350mg/ml (10.11mM)	以1 mL工作液为例，取50μL 87mg/ml的澄清DMSO储备液加到950μL玉米油中，混合均匀。工作液请现配现用！
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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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

产品质控

Bicalutamide相关产品

相关信号通路图

细胞实验数据示例

生物活性

化学信息&溶解度

实验计算

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