AR antagonist 3

Name: AR antagonist 3
Brand: TargetMol
SKU: T60719
Rating: 4.5 (1 reviews)

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产品编号 T60719Cas号 349573-58-6

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。

AR antagonist 3

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产品编号 T60719Cas号 349573-58-6

规格	价格	库存	数量
2 mg	¥ 663	5日内发货

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生物活性

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%.