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- 2025年12月05日
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- 详细信息
- 技术资料
- 保存条件：
4°C, sealed storage, away from moisture
- 英文名：
RAD1901 dihydrochloride
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1349723-93-8
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥2853.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥1156.0 |
| 规格： | 5 mg | 产品价格： | ￥2440.0 |
| 规格： | 10 mg | 产品价格： | ￥3920.0 |
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Elacestrant dihydrochloride
CAS No. : 1349723-93-8
MCE 国际站：Elacestrant dihydrochloride
产品活性：Elacestrant (RAD1901) dihydrochloride 是一种具有口服活性的选择性 estrogen receptor (ER) 降解剂 (SERD)，对 ERα 和 ERβ 的 IC50 值分别为 48 和 870 nM。Elacestrant dihydrochloride 还能有效抑制 ER+ 乳腺癌细胞系在体内外的生长。
研究领域：Vitamin D Related/Nuclear Receptor
作用靶点：Estrogen Receptor/ERR
In Vitro: Elacestrant dihydrochloride (RAD1901; 0.5 nM-10 µM; 48 h) exhibits dose-dependent inhibition of ERα expression, with a EC50 of 0.6 nM in MCF-7 cells.
Elacestrant dihydrochloride (0-1 µM; 48 h) inhibits proliferation of Estradiol (E2)-stimulated MCF-7 cells in a dose-dependent manner, with an EC50 of 4 pM.
Elacestrant dihydrochloride (0-1 µM; 24 or 48 h) results in a dose-dependent and marked decrease in estrogen receptor protein expression in MCF7, T47D, and HCC1428 cells.
Elacestrant dihydrochloride (0.01, 0.1, 1.0 µM) decreases expression of progesterone receptor (PGR, PR; an ER target gene), in both MCF7 and T47D cell lines.
In Vivo: Elacestrant dihydrochloride (0.3-120 mg/kg; p.o.; single daily for 40 days) antagonizes E2-mediated uterine stimulation in a dose-dependent manner in vivo.
Elacestrant dihydrochloride (30, 60 mg/kg; p.o.; single daily for 4 weeks) induces complete tumor growth inhibition in mice.
Tumor growth inhibition is maintained for 4 weeks after Elacestrant dihydrochloride withdrawal.
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