| 规格 | 价格 | 库存 | 数量 | 操作 |
|---|---|---|---|---|
| 1mg | ¥809.00 | 现货 | 1 | |
| 5mg | ¥1,708.00 | 现货 | 1 | |
| 10mg | ¥2,744.00 | 现货 | 1 | |
| 10mM (in 1mL DMSO) | ¥1,997.00 | 现货 | 1 |
Elacestrant (RAD1901) Dihydrochloride is an orally available selective estrogen receptor degrader (SERD) with IC50 of 48 nM and 870 nM for ERα and ERβ, respectively.
Elacestrant (RAD1901) Dihydrochloride is a selective estrogen receptor degradation (SERD), which inhibits expression of ERα and ERβ in cultured breast tumor cell lines, thus inhibits the cell proliferation in a dose-dependent manner..[1]
[1] Fiona Garner, et al. Anticancer Drugs. 2015 Oct;26(9):948-56.
Cell experiment: | For proliferation assays, MCF-7 cells are treated with 2% charcoal-stripped FBS–MEM containing 10 pM E2 with either RAD1901 or additional E2 at concentrations ranging from 10-9 to 1 M. The medium is removed after 48 h of incubation and the cells are lysed by adding 100 μl of CellTiter Glo. The plates are gently mixed on a plate shaker for 10 min before the luminescent signal is measured on a luminometer. The EC50 and IC50of the test compound are then defined[1]. |
Animal experiment: | Mice: RAD1901 is stored as a dry powder, formulated for use as a homogenous suspension in 0.5% (w/v) methylcellulose in deionized water. Fourteen days after tumor cell implantation, the mice are randomized into nine groups of 15 animals each and treated with vehicle, CI 47699 (1 mg/animal every other day), ICI 182780 (0.5 mg/animal daily), or RAD1901 (0.3, 1, 3, 10, 30, 60, 90, and 120 mg/kg daily). Tumor volumes are evaluated twice per week[1]. |
References: [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. |
