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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Androgen Receptor (AR)-AR inhibitor 1ae
AR inhibitor 1ae

Chemical Structure : AR inhibitor 1ae

CAS No.: 2920732-75-6

AR inhibitor 1ae (Compound 1ae)

货号: PC-21502Not For Human Use, Lab Use Only.

AR inhibitor 1ae is a small-molecule inhibitor of the androgen receptor activation domain (AR AD) with IC50 of 1.54 uM in androgen-induced PSA-luciferase assays, inhibits AR-V7 transcriptional activity with IC50 of 4.1 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

AR inhibitor 1ae is a small-molecule inhibitor of the androgen receptor activation domain (AR AD) with IC50 of 1.54 uM in androgen-induced PSA-luciferase assays, inhibits AR-V7 transcriptional activity with IC50 of 4.1 uM.
1ae inhibits AR-dependent targets in prostate cancer cells and is more potent in its transcriptional inhibitory effect than EPI-001 (Cat#PC-61678).
1ae significantly reduced tumor volumes in both the LNCaP and LNCaP95-D3 xenograft models.
1ae outperformed enzalutamide in the AR-V7-driven LNCaP95-D3 xenograft model of CRPC.

物理化学性质&存储条件

分子量 452.93
分子式 C26H25ClO5
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

(R)-3-(4-((6-((S)-3-chloro-2-hydroxypropoxy)-[1,1'-biphenyl]-3-yl)ethynyl)phenoxy)propane-1,2-diol

参考文献

1. Basu S, et al. Nat Struct Mol Biol. 2023 Dec 4. doi: 10.1038/s41594-023-01159-5.

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