AR antagonist 3

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

AR antagonist 3 

AR antagonist 3 是一种有效的选择性 androgen receptor (AR) 拮抗剂，IC50 为 0.47 µM。AR antagonist 3 呈剂量依赖性降低 FRET 信号 (IC50= 18.05 μM)。当瘤内给药时，AR antagonist 3 可有效抑制肿瘤生长。

AR antagonist 3

AR antagonist 3 Chemical Structure

CAS No. : 349573-58-6

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生物活性

AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally[1].

IC50 & Target

IC50: 0.47 µM (AR)[1]
体外研究
(In Vitro)

AR antagonist 3 (compound T1-12) (0.01, 0.1, 1, 10, 100 µM) shows excellent AR antagonistic activity (eGFP IC50= 0.47 μM; PSA IC50= 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 (IC50= 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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 IC50= 0.47 μM; PSA IC50= 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.

体内研究
(In Vivo)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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

Formula

C15H18N2O3S
CAS 号

349573-58-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Chai X, et al. Discovery of N-(4-(Benzyloxy)-phenyl)-sulfonamide Derivatives as Novel Antagonists of the Human Androgen Receptor Targeting the Activation Function 2. J Med Chem. 2022, 65(3):2507-2521.

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