Vepdegestrant
Based on 6 publication(s) in Google Scholar
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.
- Purity: 99.20%
- CAS No.: 2229711-68-4
- Formula: C45H49N5O4
- Molecular Weight:723.90
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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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Vepdegestrant
More
Customer Validation & Images
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Microbiological Assay
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Cell Proliferation/Viability Assay
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Flow Cytometry
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Apoptosis Analysis
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Flow Cytometry
All PROTACs Isoforms
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Biological Activity
Estrogen receptor[1]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2229711-68-4
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Appearance Solid
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Molecular Weight 723.90
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Formula C45H49N5O4
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Color White to off-white
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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
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Synonyms
ARV-471
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Shipping
Room temperature in continental US; may vary elsewhere.
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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)
Publications (6)
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Journal Impact Factor
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Most Recent
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Cancer Res
Endocrine therapy synergizes with SMAC mimetics to potentiate antigen presentation and tumor regression in hormone receptor-positive breast cancer. [Abstract]2023 Oct 2;83(19):3284-3304. PMID: 37450351
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)
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Anal Chem
Hydrogen/Deuterium Exchange for Chiral Stability Assessment in Acidic Methine-Containing Compounds. [Abstract]2025 Dec 2;97(47):26097-26107. PMID: 41243541 -
Pharmaceutics
CC-90009, a Cereblon E3 Ligase Modulator, Exhibits Antiviral Efficacy Against JEV In Vitro and In Vivo via Targeted Degradation of GSPT1 and Viral NS5 Protein. [Abstract]2025 Nov 27;17(12):1524. PMID: 41471039
Vepdegestrant purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2025 Nov 27;17(12):1524. [Abstract]
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;
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Sci Rep
Dual-drug codelivery gelatin-based hydrogel of ARV-471 and Palbociclib enhances synergistic effect in breast cancer treatment. [Abstract]2025 Nov 29. PMID: 41318792
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).
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Biomed Chromatogr
Liquid Chromatography Combined With Tandem Mass Spectrometry for the Pharmacokinetic and Metabolism Studies of PROTAC ARV-471 in Rats. [Abstract]2025 Feb;39(2):e6068. PMID: 39748262 -
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2 mg/mL (2.76 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Lin X, et al. Targeting estrogen receptor α for degradation with PROTACs: A promising approach to overcome endocrine resistance. Eur J Med Chem. 2020;206:112689. [Content Brief]
[3]. Hermida-Prado F, et al. Endocrine Therapy Synergizes with SMAC Mimetics to Potentiate Antigen Presentation and Tumor Regression in Hormone Receptor-Positive Breast Cancer. Cancer Res. 2023 Oct 2;83(19):3284-3304. [Content Brief]
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 |
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| 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 |
Vepdegestrant Related Classifications
HY-138642 Related Classifications
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