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  2. Estrogen Receptor/ERR

Elacestrant (Synonyms: RAD1901)

Cat. No.: HY-19822
Handling Instructions

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

For research use only. We do not sell to patients.

Elacestrant Chemical Structure

Elacestrant Chemical Structure

CAS No. : 722533-56-4

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

IC50: 48 nM (ERα), 870 nM (ERβ)[1]

In Vitro

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].

In Vivo

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].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1804 mL 10.9020 mL 21.8041 mL
5 mM 0.4361 mL 2.1804 mL 4.3608 mL
10 mM 0.2180 mL 1.0902 mL 2.1804 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

RAD1901 is serially diluted in ES2 screening buffer to concentrations ranging from 10 to 10-6 μM. Aliquots (25 μL) of each dilution are added to a black 384-well microtiter plate, in triplicate. The ER–Fluormone complex is prepared as directed, with 2 nM Fluormone ES2 and 30 nM ER. A 25 μL aliquot of this preparation is added to each reaction well. The plates are sealed and incubated in the dark at room temperature for 4 h. Polarization values for each well are measured and plotted against the concentration of the test compound. The IC50 is determined from at least three independent experiments, with E2 serving as a positive control[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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, tamoxifen (1 mg/animal every other day), fulvestrant (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

458.63

Formula

C₃₀H₃₈N₂O₂

CAS No.

722533-56-4

SMILES

OC1=CC=C2C[[email protected]](C3=CC=C(OC)C=C3N(CC)CC4=CC=C(CCNCC)C=C4)CCC2=C1

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Elacestrant
Cat. No.:
HY-19822
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Elacestrant

Cat. No.: HY-19822