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
CAS: 90357-06-5
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 |
相关信号通路图
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 |
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| 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 |
|---|---|---|---|---|---|
| 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 |
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) | |||
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体外溶解度 |
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 |
摩尔浓度计算器 |
|
体内溶解度 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
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
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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