|3-(4-(2-(4-(3-氯-2-羟基丙氧基)苯基)丙-2-基)苯氧基)丙烷-1,2-二醇|CsnPharm

CAS No.: 227947-06-0

EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.

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描述Androgen receptor (AR) is a member of the steroid hormone receptor family, and plays important role in the physiology and pathology of diverse tissues. EPI-001is an androgen receptor antagonist with an IC50 value of approximately 6μM for inhibition of transactivation of the androgen receptor N-terminal domain^[3]. EPI-001 (50 μM) inhibits transcriptional activity of both AR TAU1 and TAU5, and it also inhibits endogenous AR mRNA and protein expression. EPI-001(50 μM)is also a selective modulator of PPARγ in PCa cells^[4]. In vivo, EPI-001 blocks the androgen-axis and inhibits androgen-dependent tumor growth. Intravenous injection (i.v.) of EPI-001 (50mg/kg body weight) significantly reduced the weight of prostates from intact mice compared with control-treated animals. Similarly, LNCaP subcutaneous (s.c.) xenografts from intact male mice treated with EPI-001 by i.v. were significantly reduced in volume^[3].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01839760	-	-	Completed	-	United States, Illinois ... more >> Northwestern University Chicago, Illinois, United States, 60611 Australia, New South Wales Westmead Hospital Westmead, New South Wales, Australia, 2145 Australia, South Australia Royal Adelaide Hospital Adelaide, South Australia, Australia, 5000 Canada, Ontario North York General Hospital Toronto, Ontario, Canada, M2K 1E1 Mount Sinai Hospital Toronto, Ontario, Canada, M5G 1X5 Collapse <<
NCT02188004	-	-	Completed	-	China, Guangxi ... more >> Liuzhou Center of disease prevention and control Liuzhou, Guangxi, China Collapse <<
NCT02645396	-	-	Active, not recruiting	December 2018	China, Fujian ... more >> Maternity and Child care of Huli District Xiamen, Fujian, China, 361000 China, Henan Maternity and Child care of Xinmi City Zhengzhou, Henan, China, 450000 Collapse <<

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技术信息

CAS号	227947-06-0	储存条件	粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C21H27ClO5	运输	蓝冰
分子量	394.89	别名

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