PROTAC AR Degrader-4 TFA

 Cat No.: BP-400177 4.5  

PROTAC AR Degrader-4 TFA is a specialized chemical compound designed for targeted protein degradation, specifically targeting the androgen receptor (AR). This molecule is characterized by its precise binding affinity for the AR binding site, facilitating its role in PROTAC (Proteolysis Targeting Chimeras) design. It functions as a bifunctional degrader, linking the androgen receptor to an E3 ubiquitin ligase via a carefully engineered ligand. This dual interaction promotes the ubiquitination and subsequent proteasomal degradation of the AR, effectively reducing its cellular levels. The primary mechanism of action involves the recruitment of the ubiquitin-proteasome system, leading to selective degradation of the AR protein. PROTAC AR Degrader-4 TFA is invaluable in research applications focused on studying the role of AR in various biological processes and diseases, such as prostate cancer. It provides a powerful tool for elucidating the therapeutic potential of targeted protein degradation in modulating AR-driven pathways, offering insights into drug discovery and development in oncology and beyond.

PROTAC AR Degrader-4 TFA

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Category
PROTAC
Molecular Formula
C45H68F3N3O11
Molecular Weight
884.03
Appearance
Solid

* For research and manufacturing use only. Not for human or clinical use.

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Solubility
DMSO: 200 mg/mL (226.24 mM)
Appearance
Solid
Storage
Store at -80°C
IUPACName
[(5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-3-oxo-1,2,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl] 2-[2-[2-[2-[[(2S)-2-[[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]amino]-4-methylpentanoyl]amino]ethoxy]ethoxy]ethoxy]acetate;2,2,2-trifluoroacetic acid
Synonyms
PROTAC AR Degrader-4 (TFA); PROTAC AR Degrader-4 TFA; HY-111848A; MS-31636; CS-0141488
InChI Key
URZFPFDMMGLCJC-AFGPOOCPSA-N
InChI
InChI=1S/C43H67N3O9.C2HF3O2/c1-28(2)24-36(46-41(51)39(49)35(44)25-29-8-6-5-7-9-29)40(50)45-18-19-52-20-21-53-22-23-54-27-38(48)55-37-13-12-33-32-11-10-30-26-31(47)14-16-42(30,3)34(32)15-17-43(33,37)4;3-2(4,5)1(6)7/h5-9,28,30,32-37,39,49H,10-27,44H2,1-4H3,(H,45,50)(H,46,51);(H,6,7)/t30-,32-,33-,34-,35+,36-,37-,39-,42-,43-;/m0./s1
SMILES
CC(C)CC(C(=O)NCCOCCOCCOCC(=O)OC1CCC2C1(CCC3C2CCC4C3(CCC(=O)C4)C)C)NC(=O)C(C(CC5=CC=CC=C5)N)O.C(=O)(C(F)(F)F)O
Mechanism

Target: Targets androgen receptor variants, including full-length AR and AR-V7 for experimental targeted protein degradation studies.

Binding Site: Binds the AR ligand-binding or variant-associated domain and E3 ligase ligand site to support productive ternary complex formation.

Mechanism of Action: PROTAC AR Degrader-4 TFA is designed for use in PROTAC or targeted protein degradation experiments directed toward androgen receptor variants, including full-length AR and AR-V7. The bifunctional molecule links a target-recognition element to cereblon, promoting proximity between the protein of interest and ubiquitination machinery. Productive ternary-complex formation can drive polyubiquitination and proteasome-dependent target depletion, allowing researchers to compare pharmacological inhibition with protein removal. It is suitable for evaluating degradation potency, kinetics, pathway selectivity, and downstream signaling consequences in engineered or disease-relevant cellular models.

Applications

• PROTAC-Mediated AR Degradation: This product facilitates the selective degradation of androgen receptors (AR) via the ubiquitin-proteasome system. By leveraging PROTAC technology, it provides a powerful tool for researchers studying AR-related pathways, enabling the investigation of AR's role in various cellular processes and disease states.

• Targeted Protein Degradation in Cancer Research: PROTAC AR Degrader-4 TFA is instrumental in cancer research, specifically in exploring therapeutic strategies against AR-driven cancers. It allows for the precise removal of AR, aiding in the discovery of novel cancer treatment mechanisms and the assessment of AR's contribution to tumorigenesis.

• Mechanistic Studies of AR Signaling: Utilizing this PROTAC compound, researchers can dissect the intricate signaling networks involving androgen receptors. It assists in elucidating AR's interactions and downstream effects, providing insights into its biological functions and potential as a therapeutic target.

• Drug Resistance Mechanism Exploration: This product is valuable for investigating mechanisms of drug resistance associated with AR. By enabling the degradation of AR, it helps uncover resistance pathways and contributes to the development of strategies to overcome therapeutic resistance in AR-related conditions.

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Desired concentration: *

L

* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2

* Total Molecular Weight:
g/mol
Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
g/mol
g

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