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• 产品描述： ARV-771 是一种有效的 pan-(bromodomain and extra-terminal)BET 降解剂，一种新型的BET-PROTAC(proteolysis-targeting chimera)，对于BRD2(1)、BRD2(2)、BRD3(1)、BRD3(2)、BRD4(1) 和 BRD4(2)的Kd值分别为34 nM、4.7 nM、8.3 nM、7.6 nM、9.6 nM 和 7.6 nM。

• 靶点： BRD2-BD2(Cell-free assay):4.7 nM(Kd); BRD3-BD2(Cell-free assay):7.6 nM(Kd); BRD4-BD2(Cell-free assay):7.6 nM(Kd); BRD3-BD1(Cell-free assay):8.3 nM(Kd); BRD4-BD1(Cell-free assay):9.6 nM(Kd); BRD2-BD1:34 Nm;EpigeneticReaderDomain

• 体外研究：
  ARV-771 is a potent small-molecule pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved efficacy in cellular models of CRPC as compared with BET inhibition. ARV-771 treatment of CRPC cells results in apoptosis

• 体内研究：
  ARV-771 induces degradation in vivo. ARV-771 results in suppression of both AR signaling and AR levels and leads to tumor regression in a CRPC mouse xenograft model.

• 细胞实验： Cell lines: 22Rv1 cells, VCaP cells, LnCaP95 cells Concentrations: 1-300 nM Incubation Time: 24 h, 72 h Method: c-MYC ELISA. 22Rv1 cells (30,000 cells per well) were dosed with ARV-771 serially diluted at 1:3 ratio for an eight-point dose curve. AR ELISA. VCaP cells (40,000 cells per well) were dosed with ARV-771 serially diluted at 1:3 ratio for an eight-point dose curve. Cell Proliferation Assay Protocol. 22Rv1 cells (5,000 cells per well) were dosed with ARV-771 serially diluted 1:3 for a 10-point dose curve for 72 h.

• 动物实验： Animal Models: Mice implanted subcutaneously with 5 × 106 22Rv1 or VCaP cells Dosages: 30 mg/kg Administration: IH/SC

• 参考文献：
  1. Raina K, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.014 ml	5.068 ml	10.135 ml
  5 mM	0.203 ml	1.014 ml	2.027 ml
  10 mM	0.101 ml	0.507 ml	1.014 ml
  50 mM	0.02 ml	0.101 ml	0.203 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *