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AR antagonist 3 

Cat. No.: HY-144127
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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.

For research use only. We do not sell to patients.

AR antagonist 3 Chemical Structure

AR antagonist 3 Chemical Structure

CAS No. : 349573-58-6

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Description

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]

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].

MCE 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.
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].

MCE 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%.
Molecular Weight

306.38

Formula

C15H18N2O3S

CAS No.
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AR antagonist 3
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HY-144127
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