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BWA-522 is an orally available small molecule protein-targeting chimera ( PROTACs ) with significant degradation effect on AR-FL and AR-V7. BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor ( Androgen Receptor ) and induces apoptosis in PC cells. BWA-522 inhibits tumor growth in LNCaP xenograft model studies (60 mg/kg, po; TGI=76%). The efficiencies of BWA-522 in degrading AR-V7 and AR-FL were 77.3% (1 μM) and 72.0% (5 μM) in VCaP and LNCaP cells, respectively.
| CAS | 3042820-12-9 |
|---|---|
| Concentration | 10 mM in DMSO |
| Specifications & Purity | Moligand™, 10 mM in DMSO |
| Storage | Store at -80°C |
| Shipped In | Dry ice packs + Cold packs |
| Product Description | BWA-522 is an orally available small molecule protein-targeting chimera ( PROTACs ) with significant degradation effect on AR-FL and AR-V7. BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor ( Androgen Receptor ) and induces apoptosis in PC cells. BWA-522 inhibits tumor growth in LNCaP xenograft model studies (60 mg/kg, po; TGI=76%). The efficiencies of BWA-522 in degrading AR-V7 and AR-FL were 77.3% (1 μM) and 72.0% (5 μM) in VCaP and LNCaP cells, respectively. |