| 產(chǎn)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 |
| 靶點(diǎn)： |
IC50: 48 nM (ERα), 870 nM (ERβ);Estrogen/progestogenReceptor |
| 體外研究： |
Elacestrant dihydrochloride (RAD1901; 0.5 nM-10 μM; 48 h) 在 MCF-7 細(xì)胞中，以濃度依賴(lài)的方式抑制 ERα 的表達(dá) (EC50 = 0.6 nM)。 Elacestrant dihydrochloride (0-1 μM; 48 h) 以濃度依賴(lài)的方式對(duì)雌二醇 (E2) 刺激的 ER 陽(yáng)性 MCF-7 細(xì)胞顯示出抗增殖活性 (EC50 = 4 pM) 。 Elacestrant dihydrochloride (0-1 μM; 24 or 48 h) 在 MCF7, T47D 和 HCC1428 細(xì)胞中，抑制雌激素受體蛋白的表達(dá)。 Elacestrant dihydrochloride (0.01, 0.1, 1.0 μM) 能降低 MCF7 和 T47D 細(xì)胞系中孕酮受體 (PGR、PR; 一種 ER 靶基因) 的表達(dá)。 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. |
| 體內(nèi)研究： |
Elacestrant dihydrochloride (0.3-120 mg/kg; p.o.; single daily for 40 days) 在大鼠中以劑量依賴(lài)的方式拮抗 E2 介導(dǎo)的子宮刺激。 Elacestrant dihydrochloride (30, 60 mg/kg; p.o.; single daily for 4 weeks) 在小鼠體內(nèi)完全抑制腫瘤生長(zhǎng)。 Elacestrant dihydrochloride 在停藥后，還能持續(xù)四周抑制腫瘤生長(zhǎng). 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. |
| 參考文獻(xiàn)： |
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 |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
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 |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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營(yíng)業(yè)執(zhí)照(三證合一)
北京