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。

ARCC-4 is a low-nanomolar Androgen Receptor (AR) degrader based on PROTAC, with a DC 50 of 5?nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy.

Solid

VHL

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 Dmax 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.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Salami J, et al. Androgen receptor degradation by the proteolysis-targeting chimera ARCC-4 outperforms enzalutamide in cellular models of prostate cancer drug resistance. Commun Biol. 2018 Aug 2;1:100.

In Vitro: DMSO : 200 mg/mL (195.28 mM; Need ultrasonic)配制储备液