Download Files:
Products Details
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[1].
Web ID
– HY-149433
Shipping
– Room temperature
Applications
– Cancer-programmed cell death
Molecular Formula
– C43H51ClN4O7
References
– [1]Zhang B, et al. Discovery of BWA-522, a First-in-Class and Orally Bioavailable PROTAC Degrader of the Androgen Receptor Targeting N-Terminal Domain for the Treatment of Prostate Cancer. J Med Chem. 2023 Aug 24;66(16):11158-11186..
Molecular Weight
– 771.34
SMILES
– CC(C1=CC=C(OC[C@H](O)CCl)C=C1)(C)C(C=C2)=CC=C2OCC3CCN(CC4CCN(C5=CC=C6C(C(N(C7CCC(NC7=O)=O)C6=O)=O)=C5)CC4)CC3
Clinical Information
– No Development Reported
Research Area
– cancer
Solubility
– 10 mM in DMSO
Target
– Androgen Receptor;Apoptosis
Pathway
– Apoptosis;Vitamin D Related/Nuclear Receptor
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
