Elacestrant dihydrochloride
Based on 18 publication(s) in Google Scholar
Elacestrant (RAD1901) dihydrochloride is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant dihydrochloride 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.
- Purity: 99.54%
- CAS No.: 1349723-93-8
- Formula: C30H40Cl2N2O2
- Molecular Weight:531.56
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Elacestrant dihydrochloride
More- Cancer Discov. 2024 Feb 8;14(2):274-289. [Abstract]
- Cancer Res. 2024 Dec 16;84(24):4283-4297. [Abstract]
- Genes Dev. 2025 Nov 5. [Abstract]
- NPJ Breast Cancer. 2025 Nov 12;11(1):125. [Abstract]
- NPJ Breast Cancer. 2022 Dec 14;8(1):130. [Abstract]
- Biomed Pharmacother. 2024 Nov:180:117523. [Abstract]
- J Med Chem. 2020 Oct 8;63(19):11085-11099. [Abstract]
- Mol Cancer Ther. 2020 Jul;19(7):1395-1405. [Abstract]
- J Cell Mol Med. 2023 Sep;27(17):2467-2481. [Abstract]
- Biomed Chromatogr. 2026 Mar;40(3):e70374. [Abstract]
- Loyola University Chicago. 2026.
- bioRxiv. 2025 Nov 21:2025.11.20.689560. [Abstract]
- Research Square Preprint. 2024 Nov 06.
- Res Sq. 2024 Jun 04.
- bioRxiv. 2024 Jun 2:2024.05.28.596307. [Abstract]
- bioRxiv. 2023 Nov 2.
- Research Square Preprint. 2023 May 9.
- Harvard University. 2023 Mar. 30487357.
Customer Validation & Images
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Flow Cytometry
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Cell Imaging/Staining
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WB
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RT-PCR
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Flow Cytometry
Biological Activity
IC50: 48 nM (ERα), 870 nM (ERβ)[1]
Elacestrant dihydrochloride (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 dihydrochloride (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 dihydrochloride (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 dihydrochloride (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.
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Cell Line:ER-positive MCF-7 cells (Estradiol (E2)-stimulated)
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Concentration:0-1 µM
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Incubation Time:48 h
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Result:Showed antiproliferative activity on cells.
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Cell Line:MCF-7 cells
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Concentration:0.5 nM-10 µM
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Incubation Time:48 h
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Result:Inhibited ERα expression (EC50 of 0.6 nM) in a dose-dependent manner.
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Cell Line:MCF7, T47D, and HCC1428 cells
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Concentration:0-1 µM
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Incubation Time:24 or 48 h
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Result:Decreased the expression of estrogen receptor protein.
Elacestrant dihydrochloride (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 dihydrochloride withdrawal[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MCF7 cell line xenograft model of mice[2].
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Dosage:30, 60 mg/kg
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Administration:Oral administration; single daily for 4 weeks.
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Result:Inhibited growth of tumor.
Chemical Information
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CAS No. 1349723-93-8
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Appearance Solid
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Molecular Weight 531.56
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Formula C30H40Cl2N2O2
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Color White to off-white
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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
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Synonyms
RAD1901 dihydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (18)
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Journal Impact Factor
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Most Recent
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Cancer Discov
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 -
Genes Dev
Mutant p53 binds and controls estrogen receptor activity to drive endocrine resistance in ovarian cancer. [Abstract]2025 Nov 5. PMID: 41193244
Elacestrant dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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.
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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 -
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 -
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 -
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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 -
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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 -
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Solvent & Solubility
DMSO : 100 mg/mL (188.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (94.06 mM; Need ultrasonic)
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.57 mg/mL (1.07 mM); Clear solution
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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. [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]
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). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.8813 mL | 9.4063 mL | 18.8126 mL | 47.0314 mL |
| 5 mM | 0.3763 mL | 1.8813 mL | 3.7625 mL | 9.4063 mL | |
| 10 mM | 0.1881 mL | 0.9406 mL | 1.8813 mL | 4.7031 mL | |
| 15 mM | 0.1254 mL | 0.6271 mL | 1.2542 mL | 3.1354 mL | |
| 20 mM | 0.0941 mL | 0.4703 mL | 0.9406 mL | 2.3516 mL | |
| 25 mM | 0.0753 mL | 0.3763 mL | 0.7525 mL | 1.8813 mL | |
| 30 mM | 0.0627 mL | 0.3135 mL | 0.6271 mL | 1.5677 mL | |
| 40 mM | 0.0470 mL | 0.2352 mL | 0.4703 mL | 1.1758 mL | |
| 50 mM | 0.0376 mL | 0.1881 mL | 0.3763 mL | 0.9406 mL | |
| 60 mM | 0.0314 mL | 0.1568 mL | 0.3135 mL | 0.7839 mL | |
| 80 mM | 0.0235 mL | 0.1176 mL | 0.2352 mL | 0.5879 mL | |
| DMSO | 100 mM | 0.0188 mL | 0.0941 mL | 0.1881 mL | 0.4703 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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