2. PROTAC Vitamin D Related/Nuclear Receptor
  3. PROTACs Estrogen Receptor/ERR
  4. Vepdegestrant

Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM.
(Pink: ERα Target protein ligand; Blue: Cereblon ligand (HY-168055); Black: linker).

For research use only. We do not sell to patients.

CAS No. : 2229711-68-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Vepdegestrant:

Vepdegestrant Related Antibodies

Top Publications Citing Use of Products

    Vepdegestrant purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2025 Nov 27;17(12):1524.

    SH-SY5Y cells were treated with CC-90009 (10 µM), CC-92480 (5 µM), NVP-DKY709 (10 µM), ARV-110 (5 µM) or Vepdegestrant (ARV-471 ; 1 µM) and infected with JEV (MOI = 0.5) for 24 h. JEV infectivity was assessed using immunofluorescence (IF). Values were normalised to those of a dimethyl sulfoxide (DMSO) control;

    Vepdegestrant purchased from MedChemExpress. Usage Cited in: Sci Rep. 2025 Nov 29.  [Abstract]

    MCF7 and T47D cell lines were treated with Vepdegestrant (ARV-471; 10, 50, 1000 nM), Palbociclib for 72 h, followed by MTT assay.

    Vepdegestrant purchased from MedChemExpress. Usage Cited in: Sci Rep. 2025 Nov 29.  [Abstract]

    Assessment of the influence of treatment (0.5 µM Vepdegestrant (ARV-471) and 5 µM Palbociclib, for 24 h) on cell cycle phases (n = 3). All three replicates for each sample are represented as mean ± standard error of the mean (SEM). T-test analysis was performed to compare the percentage of G0/G1 phase between each treatment and control (non-treated) cells in MCF7 and T47D cancer cell lines.

    Vepdegestrant purchased from MedChemExpress. Usage Cited in: Sci Rep. 2025 Nov 29.  [Abstract]

    Assessment of treatment (0.5 µM Vepdegestrant (ARV-471) and 5 µM Palbociclib, for 72 h) on the cell death of MCF7 and T47D. Cells were classified into different populations: early apoptotic (AV-positive, PI-negative), late apoptotic (AV-positive and PI-positive) and necrotic (annexin V-negative, PI-positive).

    Vepdegestrant purchased from MedChemExpress. Usage Cited in: Cancer Res. 2023 Oct 2;83(19):3284-3304.  [Abstract]

    Histograms of MHC-I levels assessed by flow cytometry after 3 days of treatment with Fulvestrant and Vepdegestrant (ARV-471; 10, 100 nM) in the presence of IFNg for the last 24h in MCF7 cells expressing the Y537S ER mutation (ER-Y537S) under doxycycline treatment (Left). MFI quantification (Right)

    View All PROTACs Isoform Specific Products:

    View All Isoforms
    von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

    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

    Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM[1]. (Pink: ERα Target protein ligand; Blue: Cereblon ligand (HY-168055); Black: linker).

    IC50 & Target

    Estrogen receptor[1]
    In Vitro

    Vepdegestrant (10 and 100 nM, 3 days) increases MHC-I expression in MCF7 cells expressing the Y537S ER mutation (ER-Y537S)[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Vepdegestrant Related Antibodies
    In Vivo

    Vepdegestrant (3-30 mpk, p.o, daily) inhibits tumor growth in estradiol-dependent MCF7 xenografts and reduces tumor ER protein[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    723.90

    Formula

    C45H49N5O4
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C([C@@H](N(CC1=C2C=CC(N3CCN(CC4CCN(C5=CC=C([C@H]6[C@@H](C7=CC=CC=C7)CCC8=C6C=CC(O)=C8)C=C5)CC4)CC3)=C1)C2=O)CC9)NC9=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    -20°C, sealed storage, away from moisture and light

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (138.14 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 1.3814 mL 6.9070 mL 13.8141 mL
    5 mM 0.2763 mL 1.3814 mL 2.7628 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, 2 years; -20°C, 1 year (sealed storage, away from moisture and light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    Volume (start)

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    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    90% Corn Oil

      Solubility: ≥ 5.5 mg/mL (7.60 mM); Clear solution

      This protocol yields a clear solution of ≥ 5.5 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 (55.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2 mg/mL (2.76 mM); Clear solution

      This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
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    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, 2 years; -20°C, 1 year (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.
    Purity & Documentation

    Purity: 99.37% ee.: 99.68%

    SDS (393 KB)

    COA (250 KB) HNMR (838 KB) RP-HPLC (206 KB) NP-HPLC (513 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    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, 2 years; -20°C, 1 year (sealed storage, away from moisture and light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.3814 mL 6.9070 mL 13.8141 mL 34.5352 mL
    5 mM 0.2763 mL 1.3814 mL 2.7628 mL 6.9070 mL
    10 mM 0.1381 mL 0.6907 mL 1.3814 mL 3.4535 mL
    15 mM 0.0921 mL 0.4605 mL 0.9209 mL 2.3023 mL
    20 mM 0.0691 mL 0.3454 mL 0.6907 mL 1.7268 mL
    25 mM 0.0553 mL 0.2763 mL 0.5526 mL 1.3814 mL
    30 mM 0.0460 mL 0.2302 mL 0.4605 mL 1.1512 mL
    40 mM 0.0345 mL 0.1727 mL 0.3454 mL 0.8634 mL
    50 mM 0.0276 mL 0.1381 mL 0.2763 mL 0.6907 mL
    60 mM 0.0230 mL 0.1151 mL 0.2302 mL 0.5756 mL
    80 mM 0.0173 mL 0.0863 mL 0.1727 mL 0.4317 mL
    100 mM 0.0138 mL 0.0691 mL 0.1381 mL 0.3454 mL
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    Vepdegestrant 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:

    Vepdegestrant2229711-68-4ARV-471ARV471ARV 471PROTACsEstrogen Receptor/ERRoralestrogen receptorPROTACbreast cancerhetero-bifunctionalE3 ligaseubiquitylationproteasomeInhibitorinhibitorinhibit

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