不溶于水，溶于DMSO.比卡鲁胺（CDX）是一个非激素类雄激素受体（AR）拮抗剂和纯抗雄激素。它的作用通过平衡组蛋白乙酰化/脱乙酰化。比卡鲁胺（CDX）废除雄激素介导的表达。例如，MMP13在下列情况下上调，前列腺癌，PLZF（早幼粒细胞白血病锌指蛋白），和GADD45γ（生长抑制DNA损伤诱导，γ）。PI3K/AKT被雄激素磷酸化后，可抑制比卡鲁胺（CDX）的作用。

Information

Bicalutamide (ICI-176334) Bicalutamide (ICI-176334) is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy .
In vitro

Bicalutamide undergoes an antagonist-to-agonist switch, stimulating AR activity. Bicalutamide treatment of LNCaP/AR(cs) cells in absence of the synthetic androgen R1881 results in altered gene expression consistent with its well-documented agonist activity in context of AR overexpression. Bicalutamide induces cell proliferation in a dose-dependent manner, and only partially antagonized the effects of R1881. Bicalutamide treatment also results in a significant amount of nuclear AR, although less than that observed with R1881. Bicalutamide exhibits partial agonist activity as evidenced by induction of DNA binding at AR target genes and incomplete antagonism of the effects of R1881. In absence of R1881, Bicalutamide partially activates VP16-AR–mediated transcription, indicative of AR binding to DNA. In LNCaP/AR-luc cells with a stably integrates AR-driven luciferase reporter construct. In the presence of R1881, Bicalutamide shows only weak partial antagonism of VP16-AR–mediated transcription with an IC50 of 0.35 μM. Micromolar bicalutamide causes a significant dose-dependent reduction in clonogenicity. Dual inhibition of the AR and mTOR signaling pathways provides further benefit with the ridaforolimus-bicalutamide combination producing syner -gistic antiproliferative effects in prostate cancer cells in vitro when compared with each agent alone.

In vivo

Single bicalutamide reduces tumor growth by 79%, at defined submaximal doses. The ridaforolimus-bicalutamide combination exhibits improved and potent antitumor activity, almost completely abrogating tumor growth. The combination is also well tolerated, as evidenced by no significant changes in body weight over the course of treatment. Plasma PSA levels are again tightly linked to tumor growth in the combination-treated mice.
Cell Data

cell lines：

Concentrations：0-1 μM

Incubation Time：72 hours

Powder Purity:≥99%

规格

英文别名

N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methyl-propanamide

规格或纯度

Moligand™, 10mM in DMSO

英文名称

Bicalutamide (ICI-176334)

生化机理

比卡鲁胺（ICI-176334）是一种雄激素受体（AR）拮抗剂，在 LNCaP/AR(cs) 细胞系中的 IC50 值为 0.16 μM。比卡鲁胺可促进自噬。

储存条件

-80℃储存

运输条件

特低温运输

作用类型

拮抗剂

作用机制

雄激素受体拮抗剂

名称和识别符

EC号

618-534-3

分子类型

小分子

Isomeric 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

分子量

430.37

Reaxy-Rn

5364666

Reaxys-RN link address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=5364666&ln=

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高级数据

产品属性

ALogP	2.3

关联靶点（人）

AR Tclin 雄激素受体(Androgen receptor) (18 活性数据)

点击查看靶蛋白信息： AR

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

化学和物理性质

熔点

196 °C

安全和危险性（GHS）

信号词

警告

危险声明

H315: 引起皮肤刺激

H319: 引起严重眼睛刺激

H335: 可能引起呼吸道刺激

WGK Germany

RTECS

TX1413500

Merck Index

1200

个人防护装备

dust mask type N95 (US)， Eyeshields， Gloves

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技术文档和文章

Endocrinology/Hormones（内分泌与激素）在代谢调控、生殖功能与疾病研究中的应用

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探索主题:

Hormones 胰岛素 HPA轴 GPCR 内分泌激素 Endocrinology 甲状腺激素类固醇激素性激素

Applications of Endocrinology/Hormones in Metabolic Regulation, Reproductive Function, and Disease Research

目录：技术文章

探索主题:

Hormones Insulin HPA axis GPCR Endocrinology thyroid hormone steroid hormone sex hormone

此产品的引用文献

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引用文献

1. Xinyu Cheng, Xiuzhi Chen, Chengfeng Liang, Hongjun Jin, Shizhao Ren, Rongrong Xue, Fenghua Chen. (2023) Explanation and prediction for the crystallized products from amorphous bicalutamide and bicalutamide solutions by using mid-frequency Raman difference spectra. VIBRATIONAL SPECTROSCOPY, [10.1016/j.vibspec.2023.103565]
2. Jian Zhao, Nannan Liu, Shuchen Sun, Shaohua Gou, Xinyi Wang, Zhimei Wang, Xiaoyan Li, Wenjing Zhang. (2019) Light-activated ruthenium (II)-bicalutamide prodrugs for prostate cancer. JOURNAL OF INORGANIC BIOCHEMISTRY, [PMID:31054419] [10.1016/j.jinorgbio.2019.03.024]
3. Ren Yuanyuan, Cui Yue, Wang Zhen, Luo Yizhi, Jin Junchang, Yuan Yiyi, Li Xuan, Zhang Yaning, Cao Nan, Li Xiaofang, Yu Yi, Xiong Yuyan. (2025) ALDH3A2 negatively orchestrates gastric cancer progression through a synergistic induction of ferroptosis and ferroptosis-driven macrophage reprogramming. Cell Death & Disease, [PMID:41444219] [10.1038/s41419-025-08364-8]

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毕卡鲁胺, 雄激素受体拮抗剂

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