Vepdegestrant

VepdegestrantOncology
CAS: 2229711-68-4
MF: C45H49N5O4
MW: 723.9
Indications
Breast Cancer; Metastatic Breast Cancer; Solid Tumor; Metastatic Carcinoma
Therapeutic Target
ERs
Usage

A proteolysis-targeting chimera (PROTAC) estrogen receptor (ER) degrader; being developed for the treatment of ER-positive, HER2-negative locally advanced or metastatic breast cancer.

Specification
>99%
Product Description

Overview

Vepdegestrant (ARV-471) is an orally active PROTAC protein degrader of the estrogen receptor for the treatment of breast cancer. It is a heterobifunctional molecule that facilitates the interaction between estrogen receptor alpha and intracellular E3 ligase complexes.

Synonyms: ARV-471; PF-07850327

Product Categories: inhibitor; t2z001

Mol File: 2229711-68-4.mol

Physicochemical Properties

Storage temp: -20°C, sealed storage, away from moisture and light

Solubility:  DMSO: 110 mg/mL (151.95 mM; Need ultrasonic)

Form: Solid

Color: White to Off-White

MSDS Information

Experimental Data

1. Cell Experiment​​

​​DMSO:​​ 100 mg/mL (138.14 mM; Ultrasonic required)

Preparing Stock Solutions:

​​image

Please prepare the stock solution in the appropriate solvent based on the product's solubility in different solvents. Once dissolved, aliquot the solution to avoid product inactivation caused by repeated freeze-thaw cycles.

​​Storage method and shelf life of the stock solution:​​ -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light). When stored at -80°C, please use within 2 years; when stored at -20°C, please use within 1 year.


​​2. Animal Experiment​​

Please select the appropriate dissolution protocol based on your experimental animals and administration method. For the following protocols, first prepare a clear stock solution in vitro, then add co-solvents in sequence:


To ensure reliable experimental results, the clear stock solution can be stored appropriately according to the storage conditions. For in vivo experiments, it is recommended to prepare the working solution fresh and use it on the same day.

The percentages shown before the solvents refer to the volume percentage of each solvent in the final solution. If precipitation occurs during preparation, heating and/or sonication can be used to aid dissolution.


​​Protocol 1​​

Add each solvent in the following order: 10% DMSO, 90% Corn Oil

​​Solubility:​​ ≥ 5.5 mg/mL (7.60 mM); Clear solution

This protocol yields a clear solution with a concentration of ≥ 5.5 mg/mL (saturation unknown). ​​This protocol is not suitable for experiments lasting longer than half a month.​​

​​Preparation example for a 1 mL working solution:​​

Take 100 μL of the 55.0 mg/mL clear DMSO stock solution and add it to 900 μL of corn oil, mix well.


​​Protocol 2​​

Add each solvent in the following order: 10% DMSO, 40% PEG300, 5% Tween-80, 45% Saline

​​Solubility:​​ ≥ 2 mg/mL (2.76 mM); Clear solution

This protocol yields a clear solution with a concentration of ≥ 2 mg/mL (2.76 mM, saturation unknown).

​​Preparation example for a 1 mL working solution:​​

Take 100 μL of the 20.0 mg/mL clear DMSO stock solution and add it to 400 μL of PEG300, mix well. Then add 50 μL of Tween-80 to the mixture and mix thoroughly. Finally, add 450 μL of normal saline to bring the volume to 1 mL.


​​Protocol 3​​

Add each solvent in the following order: 10% DMSO, 90% (20% SBE-β-CD in Saline)

​​Solubility:​​ 2 mg/mL (2.76 mM); Suspended solution; Ultrasonic required

This protocol yields a homogeneous suspension at 2 mg/mL (2.76 mM), suitable for oral and intraperitoneal administration.

​​Preparation example for a 1 mL working solution:​​

Take 100 μL of the 20.0 mg/mL clear DMSO stock solution and add it to 900 μL of a 20% SBE-β-CD solution in saline, mix well.

Pharmacodynamics

Mechanism Of Action