Shopping Cart

Your shopping cart is currently empty

Vepdegestrant

Name: Vepdegestrant
Brand: TargetMol
SKU: T39710
Price: 186 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: Vepdegestrant) Copy Product Info

😃Good

Synonyms: Vepdegestrant

Catalog No. T39710 Copy Product Info

Purity: 99.93%

😃Good

Vepdegestrant (ARV-471) is a selective and highly potent estrogen receptor (ER, ESR1) PROTAC degrader with strong degrading activity against the ER protein. By directly degrading the ER protein rather than merely antagonizing its activity, vepdegestrant effectively inhibits the ER signaling pathway and demonstrates significant antitumor activity in ER-positive (ER⁺) breast cancer, with a DC50 value of approximately 2 nM. It is particularly effective against tumors harboring ESR1 mutations.

Cas No. 2229711-68-4

Pack Size	Price	USA Stock	Global Stock
1 mg	$186	In Stock	In Stock
5 mg	$460	In Stock	In Stock
10 mg	$655	In Stock	In Stock
25 mg	$973	In Stock	In Stock
50 mg	$1,323	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$896	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

Add to Cart

Add to Quotation

Custom-made molecule. TargetMol’s expert synthesis team delivers cost-effective solutions. Contact us for inquiries. Committed to serving you.

For research use only—not for human use. No sales to individuals. Use as intended only.

Questions

Batch Information

Select Batch

Purity:99.93%

ee:100%

Appearance:Solid

Color:White

Resource Download

COA CSFC HNMR LCMS

Product Introduction

Bioactivity

Description	Vepdegestrant (ARV-471) is a selective and highly potent estrogen receptor (ER, ESR1) PROTAC degrader with strong degrading activity against the ER protein. By directly degrading the ER protein rather than merely antagonizing its activity, vepdegestrant effectively inhibits the ER signaling pathway and demonstrates significant antitumor activity in ER-positive (ER⁺) breast cancer, with a DC50 value of approximately 2 nM. It is particularly effective against tumors harboring ESR1 mutations.
Targets & IC50	ER:1 nM (DC50)
In vitro	Methods: MCF7 cells were treated with 100 nM Vepdegestrant for 0–24 hours, followed by Western blot analysis to detect ER expression. Results: ER degradation occurred rapidly, with >80% ER degraded within 4 hours. [1]
In vivo	Methods: MCF7 breast cancer cells were orthotopically transplanted into mice. Vepdegestrant (10 mg/kg/day) was administered orally once daily for 3 consecutive days. The mice were euthanized 18 hours after dosing, and tumor tissue was collected for Western blot analysis of ER levels. Results: Vepdegestrant caused a ≥90% reduction in intratumoral ER levels. [1] Methods: MCF7, T47D, and other ER+ breast cancer cells were treated with Vepdegestrant (ARV-471) and stimulated with 10 ng/mL IFN-γ for 24 hours; cell surface MHC-I expression was detected by flow cytometry. Results: As a novel selective estrogen receptor degrader (SERD), vepdegestrant significantly reversed the inhibitory effect of estrogen on IFN-γ-induced MHC-I expression and effectively upregulated the levels of key antigen-presenting molecules.[2]
Synonyms	Vepdegestrant

Chemical Properties

Molecular Weight	723.9
Formula	C₄₅H₄₉N₅O₄
Cas No.	2229711-68-4
Smiles	OC=1C=C2C([C@H]([C@H](CC2)C3=CC=CC=C3)C4=CC=C(C=C4)N5CCC(CN6CCN(CC6)C=7C=C8C(=CC7)C(=O)N(C8)[C@@H]9C(=O)NC(=O)CC9)CC5)=CC1
Relative Density.	1.275 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 15.28 mg/mL (21.11 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (4.56 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.3814 mL	6.9070 mL	13.8141 mL	69.0703 mL
5 mM	0.2763 mL	1.3814 mL	2.7628 mL	13.8141 mL
10 mM	0.1381 mL	0.6907 mL	1.3814 mL	6.9070 mL
20 mM	0.0691 mL	0.3454 mL	0.6907 mL	3.4535 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Keywords

ubiquitylationproteasomePROTACsPROTACoralInhibitorinhibithetero-bifunctionalEstrogenReceptorEstrogen Receptor/ERRestrogen receptorERRE3 ligasebreast cancerARV-471ARV471ARV 471

Related Tags: Vepdegestrant chemical structure | Vepdegestrant in vivo | Vepdegestrant in vitro | Vepdegestrant formula | Vepdegestrant molecular weight