Art. -Nr.: HY-19822

Elacestrant

Name: Elacestrant
Brand: MedChemExpress
SKU: HY-19822
Price: 180.00 USD
Availability: InStock
Rating: 5 (19 reviews)

(Synonyms: RAD1901)

19 Cited Publications

Kundenbewertung

Based on 19 publication(s) in Google Scholar

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.

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Reinheit : 99.38%
CAS. Nr.: 722533-56-4
Formel: C₃₀H₃₈N₂O₂
Molecular Weight:458.63

Speicherung:

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)

Elacestrant Chemical Structure

CAS. Nr.: 722533-56-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (19)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 48 nM (ERα), 870 nM (ERβ)^[1]

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	EC₅₀	0.6 nM Compound: 1; RAD1901	Downregulation of ER expression in human MCF7 cells incubated for 48 hrs by ELISA Downregulation of ER expression in human MCF7 cells incubated for 48 hrs by ELISA	[PMID: 37163948]
MCF7	GI₅₀	0.028 nM Compound: RAD1901; 9	Inhibition of cell growth in human MCF7 cells after 4 days by wst-8-based colorimetric analysis Inhibition of cell growth in human MCF7 cells after 4 days by wst-8-based colorimetric analysis	[PMID: 30990042]
MCF7	IC₅₀	4.2 nM Compound: 1; RAD1901	Antiproliferative activity against estradiol-stimulated human MCF7 cells incubated for 48 hrs by CellTiter Glo assay Antiproliferative activity against estradiol-stimulated human MCF7 cells incubated for 48 hrs by CellTiter Glo assay	[PMID: 37163948]
MCF7	IC₅₀	4.2 nM Compound: 45; RAD1901	Antiproliferative activity against human MCF7 cells assessed as reduction in cell proliferation Antiproliferative activity against human MCF7 cells assessed as reduction in cell proliferation	[PMID: 33138369]
MCF7	IC₅₀	4.2 μM Compound: 8; RAD1901	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability	[PMID: 37019030]

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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 722533-56-4
Appearance Solid
Molecular Weight 458.63
Formel C₃₀H₃₈N₂O₂
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
Synonyms

RAD1901
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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)

Publications (19)

All Flow CytometryCell Imaging/StainingWBRT-PCR

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Journal Impact Factor

Cancer Discov

ESR1 F404 mutations and acquired resistance to fulvestrant in ESR1 mutant breast cancer. [Abstract]

2024 Feb 8;14(2):274-289. PMID: 37982575
Cancer Res

Induction of the TEAD Coactivator VGLL1 by Estrogen Receptor-Targeted Therapy Drives Resistance in Breast Cancer. [Abstract]

2024 Dec 16;84(24):4283-4297. PMID: 39356622
Nat Commun

ERα blockade in dendritic cells enhances antigen cross-presentation and induces antitumor CD8+ T cell immunity. [Abstract]

2026 May 5;17(1):6063. PMID: 42086580
NPJ Breast Cancer

Discovery of a novel small molecule degrader of wild type and mutant estrogen receptors using DNA encoded libraries. [Abstract]

2025 Nov 12;11(1):125. PMID: 41224743
NPJ Breast Cancer

Unconventional isoquinoline-based SERMs elicit fulvestrant-like transcriptional programs in ER+ breast cancer cells. [Abstract]

2022 Dec 14;8(1):130. PMID: 36517522
Genes Dev

Mutant p53 binds and controls estrogen receptor activity to drive endocrine resistance in ovarian cancer. [Abstract]

2025 Nov 5. PMID: 41193244

Elacestrant purchased from MedChemExpress. Usage Cited in: Genes Dev. 2025 Nov 5. [Abstract]

Elacestrant (3 µM; 48 h) induced G1 arrest of PEO1 cells stably infected with pLKO.1 and shp53.

Elacestrant purchased from MedChemExpress. Usage Cited in: Genes Dev. 2025 Nov 5. [Abstract]

Elacestrant (3 µM) inhibited the viability of PEO1-pLKO.1 and PEO1-shp53 cells grown as organoids.

Elacestrant purchased from MedChemExpress. Usage Cited in: Genes Dev. 2025 Nov 5. [Abstract]

Elacestrant (3 µM; 48 h) led to an increase in p27Kip1 protein levels in PEO1 cells transfected with siNC or sip53.

Elacestrant purchased from MedChemExpress. Usage Cited in: Genes Dev. 2025 Nov 5. [Abstract]

qPCR analysis of CDKN1B expression in PEO1 cells transfected with siNC or sip53 and treated with Elacestrant (3 µM; 48 h).

Elacestrant purchased from MedChemExpress. Usage Cited in: Genes Dev. 2025 Nov 5. [Abstract]

Elacestrant (3 µM; 48 h) arrested dramatic G1 in shp53 PEO1 cells transfected with siNC.
J Med Chem

Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. [Abstract]

2020 Oct 8;63(19):11085-11099. PMID: 32886512
Mol Cancer Ther

The Dysregulated Pharmacology of Clinically Relevant ESR1 Mutants is Normalized by Ligand-activated WT Receptor. [Abstract]

2020 Jul;19(7):1395-1405. PMID: 32381587
J Cell Mol Med

Oestrogen treatment restores dentate gyrus development in premature newborns by IGF1 regulation. [Abstract]

2023 Sep;27(17):2467-2481. PMID: 37594177
Biomed Chromatogr

Characterization of In Vitro Metabolic Profiles of Elacestrant in Rat and Human Liver Microsomes Using HPLC-MS/MS and HPLC-Q-Orbitrap-HRMS. [Abstract]

2026 Mar;40(3):e70374. PMID: 41587767
Loyola University Chicago

2026.
bioRxiv

Progesterone receptors drive advanced breast cancer phenotypes including circulating tumor- and stem-like cell expansion in the context of ESR1 mutation. [Abstract]

2025 Nov 21:2025.11.20.689560. PMID: 41332612
Research Square Preprint

2024 Nov 06.
Biomed Pharmacother

Polypharmacological profiling across protein target families and cellular pathways using the multiplexed cell-based assay platform safetyProfiler reveals efficacy, potency and side effects of drugs. [Abstract]

2024 Nov:180:117523. PMID: 39405910
Res Sq

2024 Jun 04.
bioRxiv

Targeting Unique Ligand Binding Domain Structural Features Downregulates DKK1 in Y537S ESR1 Mutant Breast Cancer Cells. [Abstract]

2024 Jun 2:2024.05.28.596307. PMID: 38854123
bioRxiv

2023 Nov 2.
Research Square Preprint

2023 May 9.
Harvard University

2023 Mar. 30487357.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

Elacestrant

19 Cited Publications

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Elacestrant

Publications Citing Use of MedChemExpress (MCE) Elacestrant

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen