2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
EXT215F4ZU
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
Degarelix is a synthetic gonadotropin-releasing hormone receptor (GNRHR) antagonist (IC50 = 3 nM in HEK293 cells expressing the human receptor).It inhibits the growth of WPMY-1, WPE1-NA22, BPH-1, and LNCaP prostate cell lines following a 72-hour incubation at a concentration of 10 μM via caspase activation and induction of apoptosis.In vivo, degarelix (2 mg/kg) decreases plasma testosterone levels in rats to castrate levels for the first 49 days post administration.It decreases tumor volume of Dunning R3327H prostate tumor flank implants in rats when administered at a dose of 1 mg/kg per month.3 Formulations containing degarelix have been used in the treatment of advanced prostate cancer.
