Home>>Signaling Pathways>> Others>> Estrogen Receptor/ERR>>Elacestrant dihydrochloride (RAD1901 dihydrochloride)
Elacestrant dihydrochloride (RAD1901 dihydrochloride) Catalog No.GC32696

Size Price Stock Qty
10mM*1mLinDMSO
$376.00
In stock
1mg
$138.00
In stock
5mg
$321.00
In stock
10mg
$459.00
In stock
50mg
$1,379.00
In stock
100mg
$1,930.00
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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & SDS

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Protocol

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.

Chemical Properties

Cas No. 1349723-93-8 SDF Download SDF
Synonyms N/A
Chemical Name N/A
Canonical SMILES OC1=CC=C2C[C@H](C3=CC=C(OC)C=C3N(CC)CC4=CC=C(CCNCC)C=C4)CCC2=C1.[H]Cl.[H]Cl
Formula C30H40Cl2N2O2 M.Wt 531.56
Solubility DMSO : 17.6 mg/mL (33.11 mM) Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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Background

Elacestrant dihydrochloride (RAD1901 dihydrochloride) is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.

RAD1901 selectively binds to and degrades the ER and is a potent antagonist of ER-positive breast cancer cell proliferation. RAD1901 treatment exhibits dose-dependent inhibition of ERα expression, with an EC50 of 0.6 nM. Treatment of ER-positive MCF-7 cells with E2 results in a potent and dose-dependent increase in proliferation, with an EC50 of 4 pM. Treatment of cells with RAD1901 in the presence of 10 pM E2 resultsin a dose-dependent decrease in proliferation, with an IC50 value of 4.2 nM[1].

RAD1901 produces a robust and profound inhibition of tumor growth in MCF-7 xenograft models. RAD1901-treated animals survived longer than those treated with either control or fulvestrant. RAD1901 preserves ovariectomy-induced bone loss and preventes the uterotropic effects of E2[1].

[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.