Elacestrant dihydrochloride (Synonyms: RAD1901 dihydrochloride)
目录号: PL04959 纯度: ≥99%
CAS No. :1349723-93-8
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中文名称
Elacestrant dihydrochloride
中文别名
Elacestrant (dihydrochloride)
英文名称
Elacestrant dihydrochloride
英文别名
Elacestrant (dihydrochloride);RAD1901 dihydrochloride;RAD-1901 dihydrochloride;Elacestrant dihydrochloride;8NZT0PR8AL;Elacestrant hydrochloride (USAN);Elacestrant hydrochloride [USAN];(R)-6-(2-(ethyl(4-(2-(ethylamino)ethyl)benzyl)amino)-4-methoxyphenyl)-5,6,7,8-tetrahydronaphthalen-2-ol dihydrochloride;Elacestrant 2HCl;Elacestrant hydrochloride;RAD1901 hydrochloride;D11672;Q27270799;(6r)-6-(2-(N-(4-(2-(ethylamino)ethyl)benzyl)-N-ethylamino;s9629;Elacestrant (RAD1901
Cas No.
1349723-93-8
分子式
C30H40Cl2N2O2
分子量
531.56
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
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。
生物活性
Elacestrant (RAD1901) dihydrochloride is an orally available and selective estrogen receptor degrader (SERD) with IC 50 s 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.
性状
Solid
IC50 & Target[1][2]
IC50: 48 nM (ERα), 870 nM (ERβ)
体外研究(In Vitro)
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。 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (188.13 mM; Need ultrasonic)H2O : 50 mg/mL (94.06 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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