产品
编 号：F283168
分子式：C21H27ClO5
分子量：394.89
分子式：C21H27ClO5
分子量：394.89
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 227947-06-0
产品详情
生物活性：
EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer.
体内研究：
EPI-00 (20 mg/kg；iv 每 5 d 一次，持续 25 d) 抑制肿瘤生长，体内无一般毒性。 EPI-00 (50 mg/kg；iv) 阻断雄激素轴并抑制雄激素依赖性肿瘤生长。Animal Model:Male NOD-SCID mice (6-8 weeks) bearing LNCaP
Dosage:20 mg/kg
Administration:I.v. every 5 days for 25 days
Result:Reduced tumors from 100.3±1.72 mm3 to 73.03±29.6 mm3 within 2 weeks.Did not cause general toxicity indicated by no change in animal behavior or body weight.
体外研究：
EPI-001 (5-100 μM；7 d) 以剂量依赖性方式抑制 PCa/CRPC 细胞生长。 EPI-001 (50 μM) 抑制内源性 AR mRNA和 PCa 和 CRPC 细胞系中的蛋白质表达。 EPI-001 (50 μM) 抑制 AR TAU1 和 TAU5 的转录活性。
EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer.
体内研究：
EPI-00 (20 mg/kg；iv 每 5 d 一次，持续 25 d) 抑制肿瘤生长，体内无一般毒性。 EPI-00 (50 mg/kg；iv) 阻断雄激素轴并抑制雄激素依赖性肿瘤生长。Animal Model:Male NOD-SCID mice (6-8 weeks) bearing LNCaP
Dosage:20 mg/kg
Administration:I.v. every 5 days for 25 days
Result:Reduced tumors from 100.3±1.72 mm3 to 73.03±29.6 mm3 within 2 weeks.Did not cause general toxicity indicated by no change in animal behavior or body weight.
体外研究：
EPI-001 (5-100 μM；7 d) 以剂量依赖性方式抑制 PCa/CRPC 细胞生长。 EPI-001 (50 μM) 抑制内源性 AR mRNA和 PCa 和 CRPC 细胞系中的蛋白质表达。 EPI-001 (50 μM) 抑制 AR TAU1 和 TAU5 的转录活性。
产品资料
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