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| Compound | ARN-509 | ||||
|---|---|---|---|---|---|
| CAS No. | 956104-40-8 | Catalog No. | T0019 | Brand | |
| Purity | 99% | Packing | 1kg | Grade | |
| Lead Time | 14Day (s) | Origin | Loading Port | ||
Apalutamide (ARN-509) is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment. Phase 3.
ARN-509 (< 10 M) inhibits androgen-mediated induction or repression of mRNA expression levels for 13 endogenous genes including PSA and TMPRSS2 in the LNCaP/AR prostate cancer cell line. ARN-509 (< 10 M) inhibits the proliferative effect of R1881 (30 pM) in the LNCaP/AR prostate cancer cell line. ARN-509 (10 M) impairs AR nuclear localization and thus reduces the concentration of AR available to bind androgen response elements (ARE) in LNCaP cells expressing AR-EYFP. ARN-509 (10 M) is able to effectively compete with R1881 (1 nM) and prevent AR from binding to promoter regions. ARN-509 inhibits R1881-induced VP16-ARmediated transcription with IC50 of 0.2 M in Hep-G2 cells expressing a VP16-AR fusion protein and an ARE-driven luciferase reporter.
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