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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)細胞系中IC50為0.16 μM。Bicalutamide 可誘導自噬。

Bicalutamide Chemical Structure

Bicalutamide Chemical Structure

CAS: 90357-06-5

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1470 現(xiàn)貨
50mg 988.18 現(xiàn)貨
200mg 3014.55 現(xiàn)貨
1g 7944.3 現(xiàn)貨
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Bicalutamide相關產(chǎn)品

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
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
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生物活性

產(chǎn)品描述 Bicalutamide是一種androgen receptor (AR)拮抗劑，在LNCaP/AR(cs)細胞系中IC50為0.16 μM。Bicalutamide 可誘導自噬。
特性 Bicalutamide 和Enzalutamide聯(lián)用治療前列腺腫瘤已經(jīng)進入二期臨床實驗階段。
靶點
Androgen Receptor [1]
(LNCaP/AR(cs) cells)
0.16 μM
體外研究(In Vitro)
體外研究活性 Bicalutamide 經(jīng)過一個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)細胞，改變基因表達，與其記錄的良好激活劑活性相符合。Bicalutamide誘導細胞增殖，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通過誘導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, Bicalutamide部分激活 VP16-AR調(diào)節(jié)的轉(zhuǎn)錄，指導AR 結(jié)合到DNA上。使用AR驅(qū)動的熒光素酶報告結(jié)構穩(wěn)定整合到LNCaP/AR-luc細胞中。在R1881存在時, 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信號通路產(chǎn)生進一步好處，在體外，Ridaforolimus-Bicalutamide聯(lián)用作用于前列腺癌細胞，與單獨藥劑處理相比，產(chǎn)生協(xié)同抗增殖效果。[3]
細胞實驗 細胞系 C4-2細胞系
濃度 0 nM-1 μM
孵育時間 72小時
方法 指數(shù)生長的C4-2細胞接種到96孔板中，在37oC下溫育過夜。24小時后，吸除其中一個板，然后儲存在-80oC中，其他使用10倍系列濃度 Ridaforolimus(1000 nM 到0.0001 nM)或乙醇（對照）處理。在 37oC下培養(yǎng)72小時，使用Cy qUANT細胞增殖檢測試劑盒測評細胞生長。
實驗圖片 檢測方法 檢測指標 實驗圖片 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處理，降低79%腫瘤生長。Ridaforolimus-Bicalutamide 聯(lián)用具有改進的和有效的抗腫瘤活性，幾乎完全廢除腫瘤生長。聯(lián)合使用具有良好耐受性，在處理過程中體重沒有明顯改變。聯(lián)用處理的小鼠中，血漿PSA水平與腫瘤生長緊密相關。[3]
動物實驗 Animal Models 攜帶C4-2細胞的雄性裸鼠
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

化學信息&溶解度

分子量 430.37 分子式

C18H14F4N2O4S
CAS號 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
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 86 mg/mL ( (199.82 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 5 mg/mL (11.61 mM)

Water : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(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，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(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：如該濃度超過該批次藥物DMSO溶解度，請先聯(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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