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ARV-471

Name: ARV-471
Brand: TargetMol
SKU: T39710
Price: 186 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰Excellent

Catalog No. T39710Cas No. 2229711-68-4

Alias Vepdegestrant

Vepdegestrant (ARV-471) is an estrogen receptor (ER) α PROTAC molecule that degrades ER in ER-positive breast cancer cell lines with a DC50 of approximately 1 nM. It can reduce the expression of classically regulated ER target genes and inhibit the growth of ER-dependent cell lines (including those expressing ESR1 variants, such as Y537S and D538G) by degrading ER.

ARV-471

🥰Excellent

Purity: 99.93%

Catalog No. T39710Alias VepdegestrantCas No. 2229711-68-4

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

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Bulk & Custom

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. However, due to objective factors, there is a small probability that the synthesis may not be successful during the R&D process. We appreciate your understanding. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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Purity:99.93%

ee:100%

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COA LCMS CSFC HNMR

Product Introduction

Bioactivity

Description	Vepdegestrant (ARV-471) is an estrogen receptor (ER) α PROTAC molecule that degrades ER in ER-positive breast cancer cell lines with a DC50 of approximately 1 nM. It can reduce the expression of classically regulated ER target genes and inhibit the growth of ER-dependent cell lines (including those expressing ESR1 variants, such as Y537S and D538G) by degrading ER.
Targets&IC50	ER:1 nM (DC50)
In vitro	Vepdegestrant (ARV-471) is an estrogen receptor (ER) α PROTAC molecule that degrades ER in ER-positive breast cancer cell lines with a DC50 of approximately 1 nM.
In vivo	Vepdegestrant (ARV-471) (3, 10, and 30 mpk/day, orally) demonstrated significant antitumor activity in estradiol-dependent MCF7 xenografts, with a greater than 90% reduction in ER protein; even more significant tumor growth inhibition (131% TGI) was observed in the MCF7 xenograft model, with a significant reduction in ER protein levels when combined with the CDK4/6 inhibitor palbociclib.[1]
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: 127 mg/mL (175.44 mM), Sonication is recommended.

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
50 mM	0.0276 mL	0.1381 mL	0.2763 mL	1.3814 mL
100 mM	0.0138 mL	0.0691 mL	0.1381 mL	0.6907 mL

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In Vivo Formulation Calculator (Clear solution)

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

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

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

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc