2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. Elacestrant

Elacestrant  (Synonyms: RAD1901)

Cat. No.: HY-19822 Purity: 99.80%
COA Handling Instructions

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Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER+ breast cancer cell lines in vitro and in vivo.

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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Based on 8 publication(s) in Google Scholar

Other Forms of Elacestrant:

Elacestrant Related Antibodies

Top Publications Citing Use of Products

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

  • Biological Activity

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  • Customer Review

Description

Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER+ breast cancer cell lines in vitro and in vivo[1][2].

IC50 & Target

IC50: 48 nM (ERα), 870 nM (ERβ)[1]
In Vitro

Elacestrant (RAD1901; 0.5 nM-10 µM; 48 h) exhibits dose-dependent inhibition of ERα expression, with a EC50 of 0.6 nM in MCF-7 cells[1].
Elacestrant (0-1 µM; 48 h) inhibits proliferation of Estradiol (E2)-stimulated MCF-7 cells in a dose-dependent manner, with an EC50 of 4 pM[1].
Elacestrant (0-1 µM; 24 or 48 h) results in a dose-dependent and marked decrease in estrogen receptor protein expression in MCF7, T47D, and HCC1428 cells[2].
Elacestrant (0.01, 0.1, 1.0 µM) decreases expression of progesterone receptor (PGR, PR; an ER target gene), in both MCF7 and T47D cell lines[2].

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

Elacestrant Related Antibodies

Cell Proliferation Assay[1]

Cell Line: ER-positive MCF-7 cells (Estradiol (E2)-stimulated)[1]
Concentration: 0-1 µM
Incubation Time: 48 h
Result: Showed antiproliferative activity on cells.

Western Blot Analysis[1]

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[2]

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.
In Vivo

Elacestrant (0.3-120 mg/kg; p.o.; single daily for 40 days) antagonizes E2-mediated uterine stimulation in a dose-dependent manner in vivo[1].
Elacestrant (30, 60 mg/kg; p.o.; single daily for 4 weeks) induces complete tumor growth inhibition in mice[2].
Tumor growth inhibition is maintained for 4 weeks after Elacestrant withdrawal[2].

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

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.
Clinical Trial
Molecular Weight

458.63

Formula

C30H38N2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC1=CC=C2C[C@H](C3=CC=C(OC)C=C3N(CC)CC4=CC=C(CCNCC)C=C4)CCC2=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 160 mg/mL (348.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 4 mg/mL (8.72 mM); Clear solution

    This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 4 mg/mL (8.72 mM); Clear solution

    This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.80%

COA (248 KB) HNMR (415 KB) LCMS (88 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1804 mL 10.9020 mL 21.8041 mL 54.5102 mL
5 mM 0.4361 mL 2.1804 mL 4.3608 mL 10.9020 mL
10 mM 0.2180 mL 1.0902 mL 2.1804 mL 5.4510 mL
15 mM 0.1454 mL 0.7268 mL 1.4536 mL 3.6340 mL
20 mM 0.1090 mL 0.5451 mL 1.0902 mL 2.7255 mL
25 mM 0.0872 mL 0.4361 mL 0.8722 mL 2.1804 mL
30 mM 0.0727 mL 0.3634 mL 0.7268 mL 1.8170 mL
40 mM 0.0545 mL 0.2726 mL 0.5451 mL 1.3628 mL
50 mM 0.0436 mL 0.2180 mL 0.4361 mL 1.0902 mL
60 mM 0.0363 mL 0.1817 mL 0.3634 mL 0.9085 mL
80 mM 0.0273 mL 0.1363 mL 0.2726 mL 0.6814 mL
100 mM 0.0218 mL 0.1090 mL 0.2180 mL 0.5451 mL
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Elacestrant Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Elacestrant722533-56-4RAD1901RAD 1901RAD-1901Estrogen Receptor/ERRbreast cancerERestrogen receptorMCF7 cellsT47D cellsHCC1428 cellsInhibitorinhibitorinhibit

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