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• 产品描述： Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC50s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis

• 靶点： hERβ：5.4 nM (IC50)；rat Erβ：3.1 nM (IC50)；mouse Erβ：3.7 nM (IC50)；hERα：1200 nM (IC50)；mouse Erα：750 nM (IC50)；rat Erα：620 nM (IC50);Estrogen/progestogenReceptor

• 体内研究：
  Prinaberel (2mg/mouse; topically; 30 min prior to UVB irradiation for 30 weeks) suppresses development of squamous cell carcinoma in SKH-1 hairless mice. Prinaberel reduces proliferation and angiogenesis and induces apoptosis in UVB-induced skin tumors. Prinaberel suppresses pro-inflammatory signaling pathway in UVB-induced skin tumors. Prinaberel diminished tumor invasiveness via PI3K-AKT pathway and WNT signaling Animal Model: Six- to eight-weeks-old SKH-1 hairless female mice Dosage: 2 mg/mouse in 200µl ethanol Administration: Topically; 30 min prior to UVB (180mJ/cm2) irradiation for 30 weeks Result: Diminished UVB-induced skin tumor development in SKH-1 hairless mice.

• 参考文献：
  1. Malamas MS, et al. Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands. J Med Chem. 2004;47(21):5021-5040. 2. Chaudhary SC, et al. Erb-041, an estrogen receptor-β agonist, inhibits skin photocarcinogenesis in SKH-1 hairless mice by downregulating the WNT signaling pathway. Cancer Prev Res (Phila). 2014;7(2):186-198. 3. Chan KKL, et al. Estrogen receptor modulators genistein, daidzein and ERB-041 inhibit cell migration, invasion, proliferation and sphere formation via modulation of FAK and PI3K/AKT signaling in ovarian cancer. Cancer Cell Int. 2018;18:65. Published 2018

• 溶解性： Soluble  in  DMSO

• 保存条件： RT

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.687 ml	18.434 ml	36.868 ml
  5 mM	0.737 ml	3.687 ml	7.374 ml
  10 mM	0.369 ml	1.843 ml	3.687 ml
  50 mM	0.074 ml	0.369 ml	0.737 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 *