Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
产品描述 | When administered intratumorally, AR antagonist 3 shows effective inhibition on the growth of tumor. AR antagonist 3 is a potent and selective antagonist of androgen receptor (AR) with an IC 50 of 0.47 μM. AR antagonist 3 dose-dependently decrease the FRET signal with an IC50 of 18.05 μM [1]. |
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%. |
分子量 | 306.38 |
分子式 | C15H18N2O3S |
CAS No. | 349573-58-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
AR antagonist 3 349573-58-6 Inhibitor inhibitor inhibit