Androgenreceptorantagonist1是一种口服有效的完整雄激素受体(AR)拮抗剂，IC50为59nM。Androgenreceptorantagonist1可用于合成PROTACAR降解剂，1μM和10μMPROTACAR降解剂作用于LNCaP细胞，分别导致24%和47%AR蛋白降解。
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.
动态评分
0.0