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Chemical Structure : BWA-522
Catalog No.: PC-21123Not For Human Use, Lab Use Only.
BWA-522 is a potent, orally bioavailable PROTAC degrader of the androgen receptor N-terminal domain (AR-NTD), induces AR-FL or AR-V7 protein degradationwith DC50 of 0.73 μM (AR-FL) and 0.67 μM (AR-V7) in VCaP cells.
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BWA-522 is a potent, orally bioavailable PROTAC degrader of the androgen receptor N-terminal domain (AR-NTD), induces AR-FL or AR-V7 protein degradationwith DC50 of 0.73 μM (AR-FL) and 0.67 μM (AR-V7) in VCaP cells.
BWA-522 is a novel and orally active AR-FL and AR-V7 PROTAC degrader.
BWA-522 inhibits the growth of AR-dependent PC cell growth, achieving IC50 values of 1.07 and 5.59 μM in LNCaP and VCaP cells.
BWA-522 effectively inhibits the growth of enzalutamide-resistant cells 22Rv1 with IC50 values of 4.08 μM, but not AR antagonist EPI-002 (IC50>30 μM).
BWA-522 suppresses the colony formation, inhibits the expression of AR-regulated protein, induced apoptosis in LNCaP and VCaP cells.
BWA-522 (20 or 60 mg/kg, PO) exhibits antitumor efficacy in the LNCaP xenograft tumor model in mice.
| M.Wt | 771.35 | |
| Formula | C43H51ClN4O7 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Bowen Zhang, et al. J Med Chem. 2023 Aug 24;66(16):11158-11186.
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