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Cat. No.: HY-138642A

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(Rac)-Vepdegestrant

(Synonyms: (Rac)-ARV-471)

(Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant 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.
(Pink: ERα Target protein ligand; Blue: Cereblon ligand (HY-138793); Black: linker).

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

CAS No.: 2229711-08-2
Formula: C₄₅H₄₉N₅O₄
Molecular Weight:723.90

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (268 KB)

(Rac)-Vepdegestrant Chemical Structure

CAS No.: 2229711-08-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity

Description

(Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant 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]. (Pink: ERα Target protein ligand; Blue: Cereblon ligand (HY-138793); Black: linker).

All PROTACs Isoforms :

All Estrogen Receptor/ERR Isoforms :

Chemical Information

CAS No. 2229711-08-2
Molecular Weight 723.90
Formula C₄₅H₄₉N₅O₄
SMILES

O=C(C(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
Synonyms

(Rac)-ARV-471
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

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Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Lin X, et al. Targeting estrogen receptor α for degradation with PROTACs: A promising approach to overcome endocrine resistance. Eur J Med Chem. 2020;206:112689. [Content Brief]

[2]. Hermida-Prado F, et al. Endocrine Therapy Synergizes with SMAC Mimetics to Potentiate Antigen Presentation and Tumor Regression in Hormone Receptor-Positive Breast Cancer. Cancer Res. 2023 Oct 2;83(19):3284-3304. [Content Brief]

[3]. JJ Flanagan, et al. Abstract P5-04-18: ARV-471, an oral estrogen receptor PROTAC degrader for breast cancer.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
Chemical Information
Purity & Documentation
References

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(Rac)-Vepdegestrant

All PROTACs Isoforms

All Estrogen Receptor/ERR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

(Rac)-Vepdegestrant Related Classifications

HY-138642A Related Classifications