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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Androgen Receptor (AR)-UT-155
UT-155

Chemical Structure : UT-155

CAS No.: 2031161-35-8

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UT-155 (UT155)

货号: PC-21406Not For Human Use, Lab Use Only.

UT-155 is a potent and selective AR degrader (SARD), binds to AR-LBD (Ki=267 nM), degrades and inhibits AR and AR splice variants (AR-SVs), including AR-V7.

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5 mg ￥2780 In stock
10 mg ￥4280 In stock
25 mg ￥7280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

UT-155 is a potent and selective AR degrader (SARD), binds to AR-LBD (Ki=267 nM), degrades and inhibits AR and AR splice variants (AR-SVs), including AR-V7.
UT-155 potently inhibits the R1881-induced wildtype AR transactivation with 6-10-fold higher potency than enzalutamide.
UT-155, but not enzalutamide, inhibits the expression of PSA in LNCaP-EnzR (F876L-AR).
UT-155 reduces AR expression and promotes degradation of the AR potentially through proteasome pathway.
UT-155 promotes degradation of splice-variants of AR in in 22RV1 cells, inhibits AR-target gene expression.
UT-155 binds to AR Activation Function Domain 1 (AF-1) between amino acids 244 and 360 with Kd of 1.32 uM, but not to the LBD.
UT-155 inhibits AR- and AR-SV-dependent PCa cell proliferation. UT-155 inhibits growth of AR-SV-dependent prostate cancer xenografts.

物理化学性质&存储条件

分子量 405.35
分子式 C20H15F4N3O2
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]-5-fluoro-α-hydroxy-α-methyl-1H-indole-1-propanamide

参考文献

1. Ponnusamy S, et al. Cancer Res. 2017 Nov 15;77(22):6282-6298.

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