Bicalutamide

别名: ICI-176334 中文名称:比卡鲁胺

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

Bicalutamide Chemical Structure

CAS: 90357-06-5

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 892.47 现货
50mg RMB 988.18 现货
200mg RMB 3014.55 现货
1g RMB 7944.3 现货
更大包装 有超大折扣

400-668-6834

info@selleck.cn

免费分装
免费预溶

客户使用Selleck的Bicalutamide发表文献53

产品质控

批次: 纯度: 99.96%
99.9

Bicalutamide相关产品

Androgen Receptor抑制剂选择性比较

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 文献信息
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
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37oC下温育过夜。24小时后,吸除其中一个板,然后储存在-80oC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 37oC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
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

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)

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

Water : Insoluble

摩尔浓度计算器

体内溶解度
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

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

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)

mg/kg g μL

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,: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: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: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。

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

* 必填项

请输入您的姓名
请输入您的邮箱地址 请输入一个有效的邮箱地址
请写点东西给我们
Tags: buy Bicalutamide | Bicalutamide ic50 | Bicalutamide price | Bicalutamide cost | Bicalutamide solubility dmso | Bicalutamide purchase | Bicalutamide manufacturer | Bicalutamide research buy | Bicalutamide order | Bicalutamide mouse | Bicalutamide chemical structure | Bicalutamide mw | Bicalutamide molecular weight | Bicalutamide datasheet | Bicalutamide supplier | Bicalutamide in vitro | Bicalutamide cell line | Bicalutamide concentration | Bicalutamide nmr
在线咨询
联系我们