AR antagonist 3

• CAT Number: I044066
• CAS Number: 349573-58-6
• Molecular Formula: C15H18N2O3S
• Molecular Weight: 306.38
• Purity: ≥95%
• Synonyms: 1-(dimethylsulfamoylamino)-4-phenylmethoxybenzene
• InChI: InChI=1S/C15H18N2O3S/c1-17(2)21(18,19)16-14-8-10-15(11-9-14)20-12-13-6-4-3-5-7-13/h3-11,16H,12H2,1-2H3
• InChIKey: VOOWYFBNDLFQKS-UHFFFAOYSA-N
• SMILES: CN(C)S(=O)(=O)NC1=CC=C(C=C1)OCC2=CC=CC=C2

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].
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].
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].

Reference

[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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