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Vepdegestrant (ARV-471) Estrogen Receptor PROTAC Degrader

Name: Vepdegestrant (ARV-471)
Brand: Selleck Chemicals
SKU: S9862
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S9862

Vepdegestrant (ARV471) is an orally bioavailable estrogen receptor-targeting (ER-targeting) PROTAC for the treatment of patients with locally advanced or metastatic ER+/HER2- breast cancer.

Vepdegestrant (ARV-471) Estrogen/progestogen Receptor chemical Chemical Structure

Quality Control

Batch: S986201 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.75%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS/MSDS
Datasheet

99.75

Related Targets	Adrenergic Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor THR PGES
Other Estrogen/progestogen Receptor Inhibitors	Elacestrant (RAD1901) Dihydrochloride MPP dihydrochloride Kaempferol Cholesterol PHTPP G15 Licochalcone A Endoxifen HCl Chrysin Pregnenolone

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (138.14 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5mg/ml (6.91mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.5mg/ml (0.69mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	723.9	Formula	C₄₅H₄₉N₅O₄	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2229711-68-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Read more about storage stability stock solution CAS number

Mechanism of Action

Targets/IC₅₀/Ki	ER
References	[1] https://pubmed.ncbi.nlm.nih.gov/32829249/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-05-06)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01042379	RECRUITING	Breast Neoplasms; Breast Cancer; Breast Tumors; Angiosarcoma; TNBC - Triple-Negative Breast Cancer; HER2-positive Breast Cancer; HER2-negative Breast Cancer; Hormone Receptor Positive Tumor; Hormone Receptor Negative Tumor; Early-stage Breast Cancer; Locally Advanced Breast Cancer	QuantumLeap Healthcare Collaborative	2010-03-01	PHASE2
NCT04606446	RECRUITING	Locally Advanced or Metastatic ER+ HER2- Breast Cancer; Locally Advanced or Metastatic Castration-resistant Prostate Cancer; Locally Advanced or Metastatic Non-small Cell Lung Cancer	Pfizer	2020-11-16	PHASE2
NCT05548127	ACTIVE_NOT_RECRUITING	Breast Cancer	Pfizer	2023-02-23	PHASE1; PHASE2
NCT06125522	ACTIVE_NOT_RECRUITING	Breast Cancer	Pfizer	2024-01-10	PHASE1; PHASE2
NCT05909397	ACTIVE_NOT_RECRUITING	Breast Cancer	Pfizer	2023-08-09	PHASE3
NCT05573555	ACTIVE_NOT_RECRUITING	Breast Cancer	Pfizer	2023-03-01	PHASE1; PHASE2

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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