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

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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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Elacestrant:

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

  • Biological Activity

  • Purity & Documentation

  • References

  • 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].

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].

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

Appearance

Solid

Formula

C30H38N2O2
CAS No.
SMILES

OC1=CC=C2C[[email protected]](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)

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
10 mM 0.2180 mL 1.0902 mL 2.1804 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.80%

COA (247 KB) HNMR (415 KB) LCMS (88 KB)

Handling Instructions (2659 KB)
References
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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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Keywords:

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

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