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Endocrinology & Hormones
Androgen Receptor antagonist
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Autophagy activator
Bicalutamide
僅限科研使用
Bicalutamide
別名: ICI-176334 中文名稱：比卡魯胺
Bicalutamide是一種androgen receptor (AR)拮抗劑，在LNCaP/AR(cs)細(xì)胞系中IC50為0.16 μM。Bicalutamide 可誘導(dǎo)自噬。
Bicalutamide Chemical Structure
CAS: 90357-06-5
Bicalutamide相關(guān)產(chǎn)品
| 相關(guān)產(chǎn)品 | Galeterone EPI-001 Cyproterone Acetate 3,3'-Diindolylmethane Bavdegalutamide (ARV-110) | 點(diǎn)擊展開(kāi) |
|---|---|---|
| 相關(guān)化合物庫(kù) | FDA藥物庫(kù) 天然產(chǎn)物庫(kù) 已知活性藥物庫(kù)-I 外泌體分泌相關(guān)化合物庫(kù) 人類激素相關(guān)化合物庫(kù) | 點(diǎn)擊展開(kāi) |
相關(guān)信號(hào)通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)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 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Bicalutamide是一種androgen receptor (AR)拮抗劑，在LNCaP/AR(cs)細(xì)胞系中IC50為0.16 μM。Bicalutamide 可誘導(dǎo)自噬。 | ||
|---|---|---|---|
| 特性 | Bicalutamide 和Enzalutamide聯(lián)用治療前列腺腫瘤已經(jīng)進(jìn)入二期臨床實(shí)驗(yàn)階段。 | ||
| 靶點(diǎn) |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | Bicalutamide 經(jīng)過(guò)一個(gè)拮抗劑到激活劑的轉(zhuǎn)變，刺激AR活性。在缺乏合成雄激素R1881的情況下，Bicalutamide處理LNCaP/AR(cs)細(xì)胞，改變基因表達(dá)，與其記錄的良好激活劑活性相符合。Bicalutamide誘導(dǎo)細(xì)胞增殖，這種作用存在劑量依賴性，且只部分抗R1881的效果。Bicalutamide 處理呀顯著產(chǎn)生大量核AR,雖然比R1881處理的少。Bicalutamide通過(guò)誘導(dǎo)DNA在AR靶基因結(jié)合，而具有部分激活劑活性，且不完全抗 R1881的效果。在R1881存在時(shí), Bicalutamide部分激活 VP16-AR調(diào)節(jié)的轉(zhuǎn)錄，指導(dǎo)AR 結(jié)合到DNA上。使用AR驅(qū)動(dòng)的熒光素酶報(bào)告結(jié)構(gòu)穩(wěn)定整合到LNCaP/AR-luc細(xì)胞中。在R1881存在時(shí), Bicalutamide只微弱且部分抗 VP16-AR調(diào)節(jié)的轉(zhuǎn)錄，IC50 為 0.35 μM。[1] 微摩爾 Bicalutamide顯著降低集落形成，這種作用存在劑量依賴性。[2] 雙重抑制 AR 和 mTOR信號(hào)通路產(chǎn)生進(jìn)一步好處，在體外，Ridaforolimus-Bicalutamide聯(lián)用作用于前列腺癌細(xì)胞，與單獨(dú)藥劑處理相比，產(chǎn)生協(xié)同抗增殖效果。[3] | |||
|---|---|---|---|---|
| 細(xì)胞實(shí)驗(yàn) | 細(xì)胞系 | C4-2細(xì)胞系 | ||
| 濃度 | 0 nM-1 μM | |||
| 孵育時(shí)間 | 72小時(shí) | |||
| 方法 | 指數(shù)生長(zhǎng)的C4-2細(xì)胞接種到96孔板中，在37oC下溫育過(guò)夜。24小時(shí)后，吸除其中一個(gè)板，然后儲(chǔ)存在-80oC中，其他使用10倍系列濃度 Ridaforolimus(1000 nM 到0.0001 nM)或乙醇（對(duì)照）處理。在 37oC下培養(yǎng)72小時(shí)，使用Cy qUANT細(xì)胞增殖檢測(cè)試劑盒測(cè)評(píng)細(xì)胞生長(zhǎng)。 | |||
| 實(shí)驗(yàn)圖片 | 檢測(cè)方法 | 檢測(cè)指標(biāo) | 實(shí)驗(yàn)圖片 | PMID |
| Western blot | Cytosolic AR / Nuclear AR |
|
30833616 | |
| Growth inhibition assay | Cell viability |
|
27994514 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | Bicalutamide按規(guī)定的次最大劑量單獨(dú)處理，降低79%腫瘤生長(zhǎng)。Ridaforolimus-Bicalutamide 聯(lián)用具有改進(jìn)的和有效的抗腫瘤活性，幾乎完全廢除腫瘤生長(zhǎng)。聯(lián)合使用具有良好耐受性，在處理過(guò)程中體重沒(méi)有明顯改變。聯(lián)用處理的小鼠中，血漿PSA水平與腫瘤生長(zhǎng)緊密相關(guān)。[3] | |
|---|---|---|
| 動(dòng)物實(shí)驗(yàn) | Animal Models | 攜帶C4-2細(xì)胞的雄性裸鼠 |
| Dosages | 10 mg/kg | |
| Administration | 口服處理 | |
| 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 |
化學(xué)信息&溶解度
| 分子量 | 430.37 | 分子式 | C18H14F4N2O4S |
| CAS號(hào) | 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 | ||
| 儲(chǔ)存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 86 mg/mL ( (199.82 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO) Ethanol : 5 mg/mL (11.61 mM) Water : Insoluble |
摩爾濃度計(jì)算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動(dòng)物體內(nèi)配方計(jì)算器 | ||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）
mg/kg
g
μL
只
第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計(jì)算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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