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首页-抗体药物偶连体和PROTACs-PROTAC-BWA-522
BWA-522

Chemical Structure : BWA-522

CAS No.: 3042820-12-9

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BWA-522 (BWA522)

货号: 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.

规格 价格 库存 数量
2 mg ￥2980 In stock
5 mg ￥4980 In stock
10 mg ￥7880 In stock
25 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 771.35
分子式 C43H51ClN4O7
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

5-(4-((4-((4-(2-(4-((S)-3-Chloro-2-hydroxypropoxy)phenyl)propan-2-yl)phenoxy)methyl)-piperidin-1-yl)methyl)piperidin-1-yl)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione

参考文献

1. Bowen Zhang, et al. J Med Chem. 2023 Aug 24;66(16):11158-11186.

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