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ARCC-4
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ARCC-4图片
CAS NO:1973403-00-7
包装与价格:
包装价格(元)
100 mg电议
500 mg电议

产品介绍

产品描述

ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide and it is a low-nanomolar androgen receptor (AR) degrader based on PROTAC, with a DC50 of 5 nM. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy[1].

体外活性

ARCC-4 selectively degrades AR via the proteasome but not PR-A or PR-B suppression[1] and it shows efficacy against clinically relevant AR mutations[1]. ARCC-4 maintains activity despite elevated androgen levels[1]. ARCC-4 enhances protein-protein interactions between AR and VHL, thereby promoting the association of the trimeric complex[1] and it induces apoptosis and inhibiting proliferation of AR-amplified prostate cancer cells[1]. ARCC-4 (0.1-10,000 nM; 20 hours) potently degrades AR with a D50 of 5?nM and Dmax of over 95%[1]. ARCC-4 (100?nM; 12 hours) shows near complete AR degradation (>98%) in prostate cancer cells[1].

Cas No.

1973403-00-7

分子式

C53H56F3N7O7S2

分子量

1024.18

储存和溶解度

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years