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].
Molecular Weight:
771.34
Formula:
C43H51ClN4O7
Target:
Apoptosis|||Androgen Receptor
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