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> Elacestrant [722533-56-4]

Elacestrant [722533-56-4]

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Referência HY-19822-1mg

Tamanho : 1mg

Marca : MedChemExpress


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]
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.

Elacestrant Related Antibodies

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.
Essai clinique
Masse moléculaire

458.63

Formule

C30H38N2O2
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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)

Solvant et solubilité
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)

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
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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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:  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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    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.
Pureté et documentation
Références

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