For research use only. Not for therapeutic Use.
BWA-522(CAT: I040723) is an orally bioavailable small-molecule PROTAC (proteolysis-targeting chimera) that effectively degrades full-length androgen receptor (AR-FL) and its splice variant AR-V7. It functions by antagonizing the androgen receptor’s N-terminal domain (AR-NTD), leading to targeted degradation and induction of apoptosis in prostate cancer (PC) cells. In cellular models, BWA-522 achieved 77.3% AR-V7 degradation at 1 μM in VCaP cells and 72.0% AR-FL degradation at 5 μM in LNCaP cells. In vivo, BWA-522 significantly inhibited tumor growth in LNCaP xenograft models (60 mg/kg, oral; TGI = 76%). It is a promising candidate for advanced prostate cancer research.
| Synonyms | 5-[4-[[4-[[4-[2-[4-[(2S)-3-chloro-2-hydroxypropoxy]phenyl]propan-2-yl]phenoxy]methyl]piperidin-1-yl]methyl]piperidin-1-yl]-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione |
| Molecular Formula | C43H51ClN4O7 |
| Purity | ≥95% |
| IUPAC Name | 5-[4-[[4-[[4-[2-[4-[(2S)-3-chloro-2-hydroxypropoxy]phenyl]propan-2-yl]phenoxy]methyl]piperidin-1-yl]methyl]piperidin-1-yl]-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione |
| InChI | InChI=1S/C43H51ClN4O7/c1-43(2,31-5-10-35(11-6-31)55-27-33(49)24-44)30-3-8-34(9-4-30)54-26-29-15-19-46(20-16-29)25-28-17-21-47(22-18-28)32-7-12-36-37(23-32)42(53)48(41(36)52)38-13-14-39(50)45-40(38)51/h3-12,23,28-29,33,38,49H,13-22,24-27H2,1-2H3,(H,45,50,51)/t33-,38?/m1/s1 |
| InChIKey | MYCPBYLZNZTLBC-OVFDOZPJSA-N |
| SMILES | CC(C)(C1=CC=C(C=C1)OCC2CCN(CC2)CC3CCN(CC3)C4=CC5=C(C=C4)C(=O)N(C5=O)C6CCC(=O)NC6=O)C7=CC=C(C=C7)OCC(CCl)O |
| Chemistry Calculators | Dilution Calculator In vivo Formulation Calculator Molarity Calculator Molecular Weight Calculator Reconstitution Calculator |
