Bicalutamide (ICI-176334) - Moligand™, 10mM in DMSO , Androgen Receptor antagonist, CAS No.90357-06-5, Androgen Receptor antagonist

CAS: 90357-06-5 Cat. No.: B407813 Molecular Weight: 430.37 EC Number: 618-534-3

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

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%

Specifications

Synonyms

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

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

ANTAGONIST

Mechanism of action

Androgen Receptor antagonist

Product Properties

• ALogP: 2.3

Names and Identifiers

• 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
• WGK Germany: 3
• RTECS: TX1413500
• Molecular Weight: 430.37
• Reaxy-Rn: 5364666
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=5364666&ln=

Associated Targets(Human)

AR Tclin Androgen receptor (18 Activities)

Discover Target: AR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Melt Point(°C): 196 °C

References

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,      [PMID:] [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]