Vepdegestrant
Product Specifications
UNSPSC 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].
Target Antigen
Estrogen Receptor/ERR; PROTACs
Type
Reference compound
Related Pathways
PROTAC;Vitamin D Related/Nuclear Receptor
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/vepdegestrant.html
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
Molecular Weight
723.90
References & Citations
[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.|[2]JJ Flanagan, et al. Abstract P5-04-18: ARV-471, an oral estrogen receptor PROTAC degrader for breast cancer.|[3]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.
Shipping Conditions
Blue Ice
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-138642/Vepdegestrant-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-138642/Vepdegestrant-SDS-MedChemExpress.pdf
CAS Number
2229711-68-4
Available Sizes
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