AR antagonist 1


Catalog No. Size PriceQuantity
M14531-2 Contact sales@xcessbio.com for quotation $100

Description

AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).

Product information

CAS Number: 1818885-54-9

Molecular Weight: 278.78

Formula: C15H19ClN2O

Chemical Name: 2-chloro-4-[(1r,3r)-3-amino-2,2,4,4-tetramethylcyclobutoxy]benzonitrile

Smiles: CC1(C)[C@@H](N)C(C)(C)[C@@H]1OC1=CC=C(C#N)C(Cl)=C1

InChiKey: ZMQAQKRIAFCCDB-JOCQHMNTSA-N

InChi: InChI=1S/C15H19ClN2O/c1-14(2)12(18)15(3,4)13(14)19-10-6-5-9(8-17)11(16)7-10/h5-7,12-13H,18H2,1-4H3/t12-,13-

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

AR antagonist 1 (compound 29) is the ligand for target ligase of ARD-266. ARD-266 is a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. AR antagonist 1 exhibits micromolar binding affinity to its E3 ligase complex, it can be successfully employed for the design of highly potent and efficient PROTAC degraders. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.

Products are for research use only. Not for human use.

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