BWA-522 is a small molecule, orally available protein-targeting chimera (PROTAC) that potentates the degradation of both full-length androgen receptor (AR-FL) and the AR-V7 splice variant. It specifically antagonizes the N-terminal domain (AR-NTD) of the androgen receptor (Androgen Receptor), prompting apoptosis in prostate cancer (PC) cells. In LNCaP xenograft models, BWA-522 demonstrated tumor growth inhibition (60 mg/kg, po, TGI=76%). The compound effectively reduced levels of AR-V7 and AR-FL by 77.3% at 1 µM and 72.0% at 5 µM, respectively, in VCaP and LNCaP cell lines [1].
Molekulargewicht:
771.34
Formel:
C43H51ClN4O7
Target-Kategorie:
Apoptosis|||Androgen Receptor
* Mehrwertsteuer und Versandkosten nicht enthalten. Irrtümer und Preisänderungen vorbehalten
