1338812-36-4
Chemical Structure
Androgen receptor antagonist 1
- CAS No.: 1338812-36-4
- Formula:C21H25ClN4O3
- Molecular Weight:416.90
IUPAC Name: N-((1r,3r)-3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl)-1-(2-hydroxyethyl)-1H-pyrazole-4-carboxamide
InChIKey: HJJNHDLYWZTKGQ-WGSAOQKQSA-N
SMILES: O=C(C1=CN(CCO)N=C1)N[C@H]2C(C)(C)[C@H](OC3=CC=C(C#N)C(Cl)=C3)C2(C)C
Biological Activity: Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM[1]. 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[2].
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Androgen receptor antagonist 1 | 99.64% | 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. | ||||||||||||||||||||
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References
- [1]. Guo C, et al. Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists. J Med Chem. 2011 Nov 10;54(21):7693-704. [Content Brief]
- [2]. Han X, et al. Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer. J Med Chem. 2019 Jan 24;62(2):941-964. [Content Brief]
