Androgen receptor antagonist 1 |
| رقم الكتالوجGC60582 |
مضاد مستقبلات الأندروجين 1 هو أحد مضادات مستقبلات الأندروجين (AR) المتوفرة عن طريق الفم مع IC 50 من 59 نانومتريمكن استخدام مناهض مستقبلات الأندروجين 1 (المركب 6) في تركيب محطلات PROTAC AR ، والتي ينتج عنها تحلل بروتين AR بنسبة 24٪ و 47٪ في خلايا LNCaP عند 1 ميكرومتر و 10 ميكرومتر على التوالي
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.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *