化合物 AR antagonist 3 T60719

Product Introduction
Bioactivity


英文名: AR antagonist 3

描述: 当 AR antagonist 3 显示出对肿瘤生长的有效抑制作用。AR antagonist 3 是雄激素受体 (AR)的选择性拮抗剂，IC50值为 0.47 μM。AR antagonist 3 以剂量依赖性的方式降低 FRET 信号 ，IC50值为 18.05 μM。

体外活性: AR antagonist 3 (compound T1-12) (0.01, 0.1, 1, 10, 100 μM) shows excellent AR antagonistic activity (eGFP IC 50 = 0.47 μM; PSA IC 50 = 1.42 μM) [1]. AR antagonist 3 (0.01, 0.1, 1, 10, 100 μM) inhibits the proliferation of LNCaP cells [1]. AR antagonist 3 (0.1, 1, 10 μM; 48 h) reduces the protein expression levels of c-Myc and KLK3 [1]. AR antagonist 3 (0.01, 0.1, 1, 10, 100 μM) exhibits a dose-dependent decrease of the FRET signal (IC 50 = 18.05 μM) [1]. AR antagonist 3 (10 μM; 2 h) reduces the DHT-mediated translocation of the AR into the nucleus in LNCaP cells [1]. Cell Viability Assay [1] Cell Line: LNCaP-ARR2PB-eGFP cells Concentration: 0.01, 0.1, 1, 10, 100 μM Incubation Time: Result: Showed excellent AR antagonistic activity (eGFP IC 50 = 0.47 μM; PSA IC 50 = 1.42 μM). Cell Proliferation Assay [1] Cell Line: LNCaP, 22Rv1, C4-2, PC3, DU145 cells Concentration: 0.01, 0.1, 1, 10, 100 μM Incubation Time: 3 days Result: Inhibited the proliferation of LNCaP cells.

体内活性: AR antagonist 3 (intratumorally injected; 2.5 mg/kg; every week for 25 days) inhibits tumor growth and the final tumor growth inhibition is 65% [1]. Animal Model: 6 weeks-old male CB17 SCID mice (specificpathogen-free grade), 18-24 g [1] Dosage: 2.5 mg/kg Administration: intratumorally injected; week; 25 days Result: Inhibited tumor growth and the final tumor growth inhibition is 65%.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途