ARCC-4,1973403-00-7

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ARCC-4

CAS No. : 1973403-00-7

MCE 国际站：ARCC-4

产品活性：ARCC-4 是基于 PROTAC 技术的，纳摩尔级的雄激素受体 (AR) 降解剂，其 D₅₀ 值为 5 nM。ARCC-4 是一种基于 enzalutamide 的 von Hippel-Lindau (VHL) 招募的 AR PROTAC。ARCC-4 能有效降解与抗雄激素研究相关的 AR 突变。

研究领域：PROTAC  |  Vitamin D Related/Nuclear Receptor

作用靶点：PROTACs  |  Androgen Receptor

In Vitro: ARCC-4 induces apoptosis and inhibiting proliferation of AR-amplified prostate cancer cells.
?ARCC-4 enhances protein-protein interactions between AR and VHL, thereby promoting the association of the trimeric complex.
?ARCC-4 (0.1-10,000 nM; 20 hours) potently degrades AR with a D₅₀ of 5?nM and D_max of over 95%.
?ARCC-4 (100?nM; 12 hours) shows near complete AR degradation (>98%) in prostate cancer cells.
?ARCC-4 selectively degrades AR via the proteasome but not PR-A or PR-B suppression.
?ARCC-4 shows efficacy against clinically relevant AR mutations.
?ARCC-4 maintains activity despite elevated androgen levels.

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