Elacestrant dihydrochloride (Synonyms: RAD1901 dihydrochloride)

Name: Elacestrant dihydrochloride
Brand: MedChemExpress
SKU: HY-19822A
Rating: 5.0 (11 reviews)

Cat. No.: HY-19822A Purity: 99.72%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

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	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 357	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 305	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 490	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1046	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1570	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2520	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Elacestrant dihydrochloride:

Elacestrant S enantiomer dihydrochloride In-stock
Elacestrant (S enantiomer) In-stock
Elacestrant Get quote

11 Publications Citing Use of MCE Elacestrant dihydrochloride

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View All Estrogen Receptor/ERR Isoform Specific Products:

View All Isoforms

Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

1349723-93-8

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
10 mM	0.1881 mL	0.9406 mL	1.8813 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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
Protocol 3

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.
Protocol 4

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.
Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 6

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.57 mg/mL (1.07 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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%

Select Batch:

Data Sheet (280 KB) SDS (252 KB)

COA (250 KB) LCMS (261 KB)

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

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.

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.

Keywords:

Elacestrant1349723-93-8RAD1901RAD 1901RAD-1901Estrogen Receptor/ERRbreast cancerERestrogen receptorMCF7 cellsT47D cellsHCC1428 cellsInhibitorinhibitorinhibit

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Elacestrant dihydrochloride (Synonyms: RAD1901 dihydrochloride)

Customer Review

Other Forms of Elacestrant dihydrochloride:

Elacestrant dihydrochloride Related Antibodies

11 Publications Citing Use of MCE Elacestrant dihydrochloride

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Estrogen Receptor/ERR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Elacestrant dihydrochloride Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Elacestrant dihydrochloride Related Classifications

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