349573-58-6
349573-58-6 structure
- Name: AR antagonist 3
- Chemical Name: AR antagonist 3
- CAS Number: 349573-58-6
- Molecular Formula: C15H18N2O3S
- Molecular Weight: 306.38
- Create Date: 2022-05-23 19:23:34
- Modify Date: 2025-08-27 15:48:57
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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[1].
| Name | AR antagonist 3 |
|---|
| 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]. |
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| Related Catalog | |
| 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]. 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]. 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%. |
| References |
| Molecular Formula | C15H18N2O3S |
|---|---|
| Molecular Weight | 306.38 |