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• 产品描述： Elacestrant (RAD1901) dihydrochloride is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant dihydrochloride also can inhibit growth of ER+ breast cancer cell lines in vitro and in vivo

• 靶点： IC50: 48 nM (ERα), 870 nM (ERβ);Estrogen/progestogenReceptor

• 体外研究：
  Elacestrant dihydrochloride (RAD1901; 0.5 nM-10 µM; 48 h) 在 MCF-7 细胞中，以浓度依赖的方式抑制 ERα 的表达 (EC50 = 0.6 nM)。 Elacestrant dihydrochloride (0-1 µM; 48 h) 以浓度依赖的方式对雌二醇 (E2) 刺激的 ER 阳性 MCF-7 细胞显示出抗增殖活性 (EC50 = 4 pM) 。 Elacestrant dihydrochloride (0-1 µM; 24 or 48 h) 在 MCF7, T47D 和 HCC1428 细胞中，抑制雌激素受体蛋白的表达。 Elacestrant dihydrochloride (0.01, 0.1, 1.0 µM) 能降低 MCF7 和 T47D 细胞系中孕酮受体 (PGR、PR; 一种 ER 靶基因) 的表达。 Cell Proliferation Assay Cell Line: ER-positive MCF-7 cells (Estradiol (E2)-stimulated) Concentration: 0-1 µM Incubation Time: 48 h Result: Showed antiproliferative activity on cells. Western Blot Analysis Cell Line: MCF-7 cells Concentration: 0.5 nM-10 µM Incubation Time: 48 h Result: Inhibited ERα expression (EC50 of 0.6 nM) in a dose-dependent manner. Western Blot Analysis Cell Line: MCF7, T47D, and HCC1428 cells Concentration: 0-1 µM Incubation Time: 24 or 48 h Result: Decreased the expression of estrogen receptor protein.

• 体内研究：
  Elacestrant dihydrochloride (0.3-120 mg/kg; p.o.; single daily for 40 days) 在大鼠中以剂量依赖的方式拮抗 E2 介导的子宫刺激。 Elacestrant dihydrochloride (30, 60 mg/kg; p.o.; single daily for 4 weeks) 在小鼠体内完全抑制肿瘤生长。 Elacestrant dihydrochloride 在停药后，还能持续四周抑制肿瘤生长. Animal Model: MCF7 cell line xenograft model of mice[2]. Dosage: 30, 60 mg/kg Administration: Oral administration; single daily for 4 weeks. Result: Inhibited growth of tumor.

• 参考文献：
  1. Garner F, et al. RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models. Anticancer Drugs. 2015 Oct;26(9):948-56. 2. Bihani T, et al. Elacestrant (RAD1901), a Selective Estrogen Receptor Degrader (SERD), Has Antitumor Activity in Multiple ER+ Breast Cancer Patient-derived Xenograft Models. Clin Cancer Res. 2017 Aug 15;23(16):4793-4804.

• 溶解性： Soluble  in  DMSO、H2O

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.881 ml	9.406 ml	18.813 ml
  5 mM	0.376 ml	1.881 ml	3.763 ml
  10 mM	0.188 ml	0.941 ml	1.881 ml
  50 mM	0.038 ml	0.188 ml	0.376 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 *