Androgen receptor antagonist 1 |
| Catalog No.GC60582 |
L'antagoniste des récepteurs aux androgènes 1 est un antagoniste complet des récepteurs aux androgènes (AR) disponible par voie orale avec une IC50 de 59 nM. L'antagoniste des récepteurs aux androgènes 1 (composé 6) peut être utilisé dans la synthèse des dégradeurs PROTAC AR, ce qui entraÎne une dégradation de la protéine AR de 24 % et 47 % dans les cellules LNCaP À 1 μM et 10 μM, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1338812-36-4
Sample solution is provided at 25 µL, 10mM.
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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].
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[1]. Cell Proliferation Assay[1] Cell Line: Prostate cancer (CaP) cells (LNCAP, LNAR, and DU145)
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[1]. Animal Model: Male athymic nude mice with LNCaP xenograft model of CRPC[1]
[1]. Guo C, et al. Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists. J Med Chem. 2011 Nov 10;54(21):7693-704. [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.
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)
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