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

Vepdegestrant  (Synonyms: ARV-471)

Cat. No.: HY-138642 Purity: 99.60%
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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.

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

Vepdegestrant Chemical Structure

Vepdegestrant Chemical Structure

CAS No. : 2229711-68-4

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1 mg USD 324 In-stock
5 mg USD 810 In-stock
10 mg USD 1200 In-stock
25 mg USD 2400 In-stock
50 mg USD 3850 In-stock
100 mg USD 6150 In-stock
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Based on 2 publication(s) in Google Scholar

Other Forms of Vepdegestrant:

Vepdegestrant Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All Estrogen Receptor/ERR Isoform Specific Products:

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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].

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.

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  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

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
(per animal)

μL

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: 99.60%

SDS (393 KB)

COA (250 KB) HNMR (262 KB) LCMS (268 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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