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

Elacestrant dihydrochloride  (Synonyms: RAD1901 dihydrochloride)

Cat. No.: HY-19822A Purity: 99.72%
COA Handling Instructions

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.

Elacestrant dihydrochloride Chemical Structure

Elacestrant dihydrochloride Chemical Structure

CAS No. : 1349723-93-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 357 In-stock
Solution
10 mM * 1 mL in DMSO USD 357 In-stock
Solid
1 mg USD 150 In-stock
5 mg USD 305 In-stock
10 mg USD 490 In-stock
50 mg USD 1570 In-stock
100 mg USD 2520 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Elacestrant dihydrochloride:

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  • Biological Activity

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  • References

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Description

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[1][2].

IC50 & Target

IC50: 48 nM (ERα), 870 nM (ERβ)[1]

In Vitro

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.

Cell Proliferation Assay[1]

Cell Line: ER-positive MCF-7 cells (Estradiol (E2)-stimulated)
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 dihydrochloride (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 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.

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

531.56

Formula

C30H40Cl2N2O2

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.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8813 mL 9.4063 mL 18.8126 mL
5 mM 0.3763 mL 1.8813 mL 3.7625 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). 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.

  • Molarity Calculator

  • Dilution Calculator

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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: ≥ 2.87 mg/mL (5.40 mM); Clear solution

  • Protocol 2

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.87 mg/mL (5.40 mM); Clear solution

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.72%

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). 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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Elacestrant dihydrochloride 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.

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Elacestrant dihydrochloride
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