Description

Product Description

Bicalutamide (CAS 90357-06-5) is a potent, selective, non-steroidal androgen receptor (AR) antagonist that blocks the androgen-mediated activation of gene transcription. It has become an essential reference compound in prostate cancer research, particularly in studies exploring androgen receptor regulation, hormonal feedback mechanisms, and resistance pathways to antiandrogen therapy.

In preclinical research, Bicalutamide functions by binding to the ligand-binding domain of the androgen receptor, thereby preventing the natural ligand—testosterone or dihydrotestosterone (DHT)—from activating downstream transcriptional activity. This blockade effectively inhibits androgen-dependent cell proliferation and survival signaling in prostate and other androgen-sensitive cells. The compound is widely employed in both in vitro and in vivo models to elucidate molecular mechanisms governing hormone receptor dynamics, cell cycle progression, and apoptosis induction.

Bicalutamide’s versatility as a research reagent stems from its ability to modulate androgen receptor signaling in multiple biological contexts. Researchers employ it to study androgen receptor coactivators, nuclear translocation, gene regulation, and the emergence of antiandrogen-resistant receptor variants (e.g., AR-V7). These investigations contribute to understanding how tumor cells adapt to prolonged AR inhibition, offering insights into next-generation inhibitor development.

From a chemical standpoint, Bicalutamide is a racemic mixture where the R-enantiomer exhibits primary biological activity. The compound’s structure (C18H14F4N2O4S, molecular weight 430.37 g/mol) enables high receptor affinity and selective antagonism without intrinsic androgenic activity. It is characterized by a high degree of lipophilicity, facilitating receptor binding and intracellular distribution in model systems.

Supplied as a white crystalline powder with purity ≥99%, Bicalutamide is highly stable under refrigerated storage conditions (2–8 °C). It is soluble in DMSO, ethanol, and slightly in methanol, which allows flexible preparation for cell culture and animal model experiments. The compound’s analytical identity is verified by HPLC, mass spectrometry (MS), and nuclear magnetic resonance (NMR), ensuring reproducibility across research applications.

Bicalutamide’s impact in research extends beyond prostate cancer models. It is frequently used to investigate androgen-dependent signaling in other tissues, such as muscle, skin, and endocrine glands. Moreover, it serves as a valuable tool in the development and validation of AR-targeting molecular probes, receptor degradation enhancers, and structure-based drug design platforms. The compound’s well-documented pharmacological profile and extensive use in literature make it a gold-standard reagent for exploring androgen biology and endocrine modulation.

Its role in molecular and cellular research is complemented by its use in biochemical assays to quantify androgen receptor occupancy, ligand-binding kinetics, and receptor conformation changes. Advanced imaging studies also utilize Bicalutamide to observe AR localization and trafficking dynamics. With its non-steroidal nature, high receptor selectivity, and reproducible antagonistic activity, Bicalutamide remains an indispensable compound for mechanistic studies of androgen receptor signaling, tumor progression, and endocrine feedback regulation.

Product Specifications 

Mechanism of Action

Bicalutamide functions as a competitive non-steroidal antagonist of the androgen receptor (AR). The androgen receptor is a ligand-activated transcription factor that mediates the biological effects of androgens such as testosterone and dihydrotestosterone (DHT). By binding to the ligand-binding domain of the AR, Bicalutamide blocks the receptor’s activation and prevents the recruitment of transcriptional coactivators necessary for target gene expression.

Upon binding, Bicalutamide induces a conformational change in the androgen receptor, stabilizing it in an inactive form that fails to translocate efficiently into the nucleus or bind to androgen response elements (AREs) on DNA. This disruption halts transcription of androgen-responsive genes responsible for cell proliferation, survival, and differentiation.

In prostate cancer models, Bicalutamide’s inhibitory action reduces androgen-dependent tumor growth and induces apoptosis. It also provides an effective means to model androgen deprivation resistance, a common phenomenon in long-term androgen receptor blockade. Prolonged exposure to Bicalutamide in laboratory models has revealed adaptive mechanisms such as receptor overexpression, mutations in the ligand-binding domain, and emergence of splice variants (notably AR-V7), which maintain receptor activity despite antagonist presence.

Bicalutamide’s downstream impact involves several signaling cascades, including the PI3K/AKT, MAPK/ERK, and NF-κB pathways. Through AR inhibition, it indirectly modulates these signaling networks, thereby affecting metabolic regulation, cellular stress responses, and gene transcription. This complex interplay makes Bicalutamide an invaluable research tool in systems biology and molecular pharmacology, where the goal is to map feedback loops between hormonal and intracellular signaling processes.

Researchers often employ Bicalutamide to:

• Evaluate androgen receptor target gene suppression (e.g., PSA, TMPRSS2).

• Examine AR nuclear localization and chromatin binding dynamics.

• Investigate AR resistance mechanisms at the molecular and cellular level.

• Compare selective androgen receptor modulators (SARMs) against known antagonists.

• Validate computational or structure-based docking models for AR-ligand interactions.

Because of its high affinity and specificity, Bicalutamide continues to serve as the benchmark antagonist for AR functional studies, resistance evolution modeling, and drug–target interaction profiling.

Side Effects

In preclinical research environments, Bicalutamide should be treated as a bioactive compound requiring proper safety precautions.

• Avoid inhalation, ingestion, and direct skin or eye contact.

• Use gloves, lab coat, and protective eyewear when handling.

• Conduct all experiments in a well-ventilated fume hood.

• Dispose of contaminated materials according to institutional and environmental regulations.

• Store between 2–8 °C in a dry, light-protected environment.

Bicalutamide is provided strictly for laboratory use only. It is not intended for human or veterinary applications. Observed effects during animal research (e.g., hormone suppression, hepatic enzyme modulation, or endocrine imbalance) are valuable data points for experimental design but should not be interpreted as clinical side effects.

Keywords

Bicalutamide, CAS 90357-06-5, non-steroidal antiandrogen, androgen receptor antagonist, prostate cancer research, endocrine signaling, hormonal blockade, AR pathway inhibition, small molecule inhibitor, laboratory reagent, ≥99% purity, factory peptide supplier, peptide wholesale China, China peptide manufacturer, OEM & bulk peptide production, high purity research compound.

Shipping Guarantee

All shipments are managed using validated cold-chain logistics to maintain compound integrity. Each order is sealed in moisture-proof, light-resistant containers with secondary protective wrapping. Real-time temperature monitoring ensures stability during transit. Packages are shipped via international express couriers with full tracking and insurance coverage, ensuring prompt and secure delivery for global laboratories.

Trade Assurance

We guarantee product authenticity and analytical verification (HPLC, MS, NMR). Each batch of Bicalutamide is accompanied by a Certificate of Analysis (CoA) verifying ≥99% purity and identity. Our trade assurance policy covers replacement or refund for any deviations from listed specifications, ensuring consistent quality and reproducibility for research institutions.

Payment Support

Flexible and secure payment solutions are available for global research clients. Accepted methods include PayPal, major credit cards (Visa, MasterCard, American Express), telegraphic transfer (T/T), and cryptocurrencies (USDT, Bitcoin, Ethereum). All payments are protected by advanced encryption and verified gateways to maintain confidentiality and transaction security.

Disclaimer

This product is intended for laboratory research use only. It is not intended for human or veterinary administration. All users must be qualified researchers familiar with handling small molecule inhibitors and bioactive compounds. Data derived from research use of this product must not be interpreted as clinical evidence or therapeutic advice.