AR antagonist 3

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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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