Vepdegestrant (ARV471)

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 (ARV471) Chemical Structure

Vepdegestrant (ARV471) Chemical Structure

CAS: 2229711-68-4

Purity & Quality Control

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

Vepdegestrant (ARV471) Related Products

Choose Selective Estrogen/progestogen Receptor Inhibitors

Biological Activity

Description 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.
Targets
ER [1]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06125522 Not yet recruiting
Breast Cancer
Pfizer|Arvinas Estrogen Receptor Inc.|Carrick Therapeutics Limited
November 10 2023 Phase 2
NCT05930925 Completed
Healthy
Pfizer|Arvinas Estrogen Receptor Inc.
June 12 2023 Phase 1
NCT05654623 Recruiting
Advanced Breast Cancer
Pfizer|Arvinas Estrogen Receptor Inc.
March 3 2023 Phase 3
NCT05573555 Recruiting
Breast Cancer
Pfizer|Arvinas Estrogen Receptor Inc.
March 1 2023 Phase 2

Chemical Information & Solubility

Molecular Weight 723.9 Formula

C45H49N5O4

CAS No. 2229711-68-4 SDF --
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (138.14 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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