产品信息
抗原名称
Androgen Receptor
商品描述
ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM, useful for prostate cancer treatment.
分子量
477.43
纯度
>98%
可溶性
DMSO 18 mg/mL (37.7 mM)
Ethanol 5 mg/mL (10.47 mM)
Ethanol 5 mg/mL (10.47 mM)
外观
Powder
In vitro(体外研究)
ARN-509 (
In vivo(体内研究)
ARN-509 (10 mg/kg/d, oral) inhibits tumor growth with decreased proliferative index and increased apoptotic rate in castrate male immunodeficient mice harboring LNCaP/AR-luc xenograft tumors. ARN-509 dose dependently inhibits tumor growth with highest efficacy at dose of 30 mg/kg/day in castrate male immunodeficient mice harboring LNCaP/AR-luc xenograft tumors. ARN-509 dosed at 10 mg/kg/d for 28 days results in a 3-fold reduction in prostates weight associated with lacking glandular secretory activity and 1.7-fold reduction in epididymis weight in adult male dogs. ARN-509 (10 mg/kg/d, oral) inhibits cell proliferation of prostate tissues in adult male dogs. ARN-509 is safe and well tolerated in 24 patients with metastatic CRPC who has progressed on prior treatments and peak plasma concentrations occurred 2 to 3 hours after administration. ARN-509 results in durable PSA declines at doses ranging from 30 to 300 mg in patients with metastatic CRPC. ARN-509 shows powerful anti-cancer activity and induces durable remissions long after therapy completion in castrate resistant prostate cancer mouse models.
背景
别名
ARN 509; ARN-509
分子式
C21H15F4N5O2S
CAS号
956104-40-8
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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