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

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.

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CAS No. : 722533-56-4

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
1 mg 해외재고보유
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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고객리뷰

Based on 17 publication(s) in Google Scholar

Other Forms of Elacestrant:

Top Publications Citing Use of Products

    Elacestrant 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 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 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 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 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.

    View All Estrogen Receptor/ERR Isoform Specific Products:

    • Biological Activity

    • 순도&문서

    • References

    • 고객리뷰

    제품 설명

    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.

    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.
    Clinical Trial
    분자량

    458.63

    화학식

    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

    선적

    Room temperature in continental US; may vary elsewhere.

    보관

    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)

    용액&용해도
    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.

    • 몰농도 계산기

    • 농도 희석 계산기

    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:  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.
    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.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    순도&문서

    Purity: 99.38%

    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 and light). 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
    DMSO 1 mM 2.1804 mL 10.9020 mL 21.8041 mL 54.5102 mL
    5 mM 0.4361 mL 2.1804 mL 4.3608 mL 10.9020 mL
    10 mM 0.2180 mL 1.0902 mL 2.1804 mL 5.4510 mL
    15 mM 0.1454 mL 0.7268 mL 1.4536 mL 3.6340 mL
    20 mM 0.1090 mL 0.5451 mL 1.0902 mL 2.7255 mL
    25 mM 0.0872 mL 0.4361 mL 0.8722 mL 2.1804 mL
    30 mM 0.0727 mL 0.3634 mL 0.7268 mL 1.8170 mL
    40 mM 0.0545 mL 0.2726 mL 0.5451 mL 1.3628 mL
    50 mM 0.0436 mL 0.2180 mL 0.4361 mL 1.0902 mL
    60 mM 0.0363 mL 0.1817 mL 0.3634 mL 0.9085 mL
    80 mM 0.0273 mL 0.1363 mL 0.2726 mL 0.6814 mL
    100 mM 0.0218 mL 0.1090 mL 0.2180 mL 0.5451 mL
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      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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    상품명:
    Elacestrant
    Cat. No.:
    HY-19822
    수량:
    MCE Japan Authorized Agent: