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Cat. No.: HY-138642B

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rel-Vepdegestrant

Name: rel-Vepdegestrant
Brand: MedChemExpress
SKU: HY-138642B
Availability: PreOrder

(Synonyms: rel-ARV-471; rel-PF-07850327)

(Rac)-Vepdegestrant is the relative configuration 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.: 2614417-52-4
Formula: C₄₅H₄₉N₅O₄
Molecular Weight:723.90

Storage:

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

rel-Vepdegestrant Chemical Structure

CAS No.: 2614417-52-4

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Fluorescent Dye

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

Biological Activity

Description

(Rac)-Vepdegestrant is the relative configuration 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. 2614417-52-4
Molecular Weight 723.90
Formula C₄₅H₄₉N₅O₄
SMILES

OC1=CC=C([C@@H](C2=CC=C(N3CCC(CC3)CN4CCN(C5=CC=C(C(N([C@@H]6C(NC(CC6)=O)=O)C7)=O)C7=C5)CC4)C=C2)[C@@H](C8=CC=CC=C8)CC9)C9=C1
Synonyms

rel-ARV-471; rel-PF-07850327
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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