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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Androgen Receptor (AR)-UT-34
UT-34

Chemical Structure : UT-34

CAS No.: 2168525-92-4

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UT-34 (UT34)

货号: PC-21405Not For Human Use, Lab Use Only.

UT-34 is a potent, second-generation androgen receptor (AR) pan antagonist, degrades enzalutamide-sensitive and -resistant ARs and AR splice variants (AR-SVs).

规格 价格 库存 数量
10 mg ￥1980 In stock
25 mg ￥2980 In stock
50 mg ￥4780 In stock
100 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

UT-34 is a potent, second-generation androgen receptor (AR) pan antagonist, degrades enzalutamide-sensitive and -resistant ARs and AR splice variants (AR-SVs).
UT-34 interacts with AR AF-1 domain, UT-34 does not bind to the AR-LBD.
UT-34 antagonizes the wild-type AR with IC50 of 200 nM, inhibits the various mutant ARs (W741L, T877A, and F876L) comparably or with better IC50.
UT-34 downregulates T877A-AR and F876L-enzalutamide-resistant AR, reduces AR levels at 1 uM in LNCaP and MR49F cells.
UT-34 does not inhibit the transactivation of GR and mineralocorticoid receptor, and does not downregulate the ER and PR protein levels.
UT-34 requires ubiquitin proteasome pathway to degrade the AR.
UT-34 promotes AR-V7 degradation, inhibits AR and AR-V7-target gene expression and induces distinct AR conformation.
UT-34 inhibits enzalutamide-sensitive and -resistant AR-dependent gene expression and prostate cancer cell proliferation.
UT-34 inhibits AR function and proliferation of an AR-amplified model (VCaP cells) and a PDX model.

物理化学性质&存储条件

分子量 356.28
分子式 C15H12F4N4O2
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

(αS)-N-[4-Cyano-3-(trifluoromethyl)phenyl]-4-fluoro-α-hydroxy-α-methyl-1H-pyrazole-1-propanamide

参考文献

1. Ponnusamy S, et al. Clin Cancer Res. 2019 Nov 15;25(22):6764-6780.

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