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Chemical Structure : Apalutamide
CAS No.: 956104-40-8
Catalog No.: PC-73182Not For Human Use, Lab Use Only.
Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist with binding IC50 of 16 nM.
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Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist with binding IC50 of 16 nM.
Apalutamide (ARN-509) targets the AR ligand-binding domain and prevents AR nuclear translocation, DNA binding, and transcription of AR gene targets, inhibits AR transcriptional activity and prostate cancer cell proliferation.
ARN-509 lacked significant agonist activity in preclinical models of CRPC compared to bicalutamide.
ARN-509 showed greater efficacy than MDV3100 in a clinically valid murine xenograft model of human CRPC.
| M.Wt | 477.43 | |
| Formula | C21H15F4N5O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
4-(7-(6-Cyano-5-(trifluoromethyl)pyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl)-2-fluoro-N-methylbenzamide |
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1. Joseph JD, et al. Cancer Discov. 2013 Sep;3(9):1020-9.
2. Clegg NJ, et al. Cancer Res. 2012 Mar 15;72(6):1494-503.
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