Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.

Product information

CAS Number: 1338812-36-4

Molecular Weight: 416.90

Formula: C21H25ClN4O3

Chemical Name: N-[3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]-1-(2-hydroxyethyl)-1H-pyrazole-4-carboxamide

Smiles: CC1(C)C(NC(=O)C2C=NN(CCO)C=2)C(C)(C)C1OC1=CC(Cl)=C(C=C1)C#N

InChiKey: HJJNHDLYWZTKGQ-UHFFFAOYSA-N

InChi: InChI=1S/C21H25ClN4O3/c1-20(2)18(25-17(28)14-11-24-26(12-14)7-8-27)21(3,4)19(20)29-15-6-5-13(10-23)16(22)9-15/h5-6,9,11-12,18-19,27H,7-8H2,1-4H3,(H,25,28)

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:

Androgen receptor antagonist 1 (Compound 26; 1 nM-100 μM) shows significant cell growth inhibition effects for LNCaP and LNAR cells but not DU145 cells.

In Vivo:

Androgen receptor antagonist 1 (Compound 26; 100 mg/kg once a day for 5 weeks) demonstrates excellent in vivo tumor growth inhibition upon oral administration in a castration-resistant prostate cancer (CRPC) animal model.

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