Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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].
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]. |
分子量 | 1024.18 |
分子式 | C53H56F3N7O7S2 |
CAS No. | 1973403-00-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
ARCC-4 1973403-00-7 Others ARCC 4 ARCC4 Inhibitor inhibitor inhibit