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Art. -Nr.: 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).

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CAS. Nr.: 2614417-52-4
Formel: C₄₅H₄₉N₅O₄
Molecular Weight:723.90

Speicherung:

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

rel-Vepdegestrant Chemical Structure

CAS. Nr.: 2614417-52-4

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Chemical Information
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Biologische Aktivität

Beschreibung

(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).

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	IC₅₀	2.7 nM Compound: 7; ARV-471	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo reagent based luminescence analysis Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo reagent based luminescence analysis	[PMID: 39610216]
MCF7	IC₅₀	133 nM Compound: 7; ARV-471	Antiproliferative activity against human MCF7 cells harboring ER-alpha Y537S mutant assessed as inhibition of cell growth Antiproliferative activity against human MCF7 cells harboring ER-alpha Y537S mutant assessed as inhibition of cell growth	[PMID: 39610216]

Chemical Information

CAS. Nr. 2614417-52-4
Molecular Weight 723.90
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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