Product Data Sheet

(Rac)-Vepdegestrant

Catalog No. A84570

main product photo
(Rac)-Vepdegestrant targets the estrogen receptor (ER) as a PROTAC (proteolysis-targeting chimera) degrader, effectively inducing the proteasomal degradation of estrogen receptors in breast cancer cells. This hetero-bifunctional compound enhances the interaction between ER-alpha and an E3 ligase complex, resulting in significant ubiquitylation. (Rac)-Vepdegestrant exhibits potent biological activity, showcasing a half-maximal degradation concentration (DC50) of approximately 2 nM in ER-positive breast cancer cell lines, making it a valuable tool for studying ER-related signaling pathways and potential therapeutic applications in breast cancer research.
Chemical Information
Catalog NumA84570
M. Wt723.90
FormulaC45H49N5O4
Purity>98%
Storageat -20 °C 3 years (powder form); at -20 °C 6 months (Solution base)
CAS No.2229711-08-2
Synonyms(Rac)-ARV-471
SMILESO=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
Biological Activity
Description(Rac)-Vepdegestrant targets the estrogen receptor (ER) as a PROTAC (proteolysis-targeting chimera) degrader, effectively inducing the proteasomal degradation of estrogen receptors in breast cancer cells. This hetero-bifunctional compound enhances the interaction between ER-alpha and an E3 ligase complex, resulting in significant ubiquitylation. (Rac)-Vepdegestrant exhibits potent biological activity, showcasing a half-maximal degradation concentration (DC50) of approximately 2 nM in ER-positive breast cancer cell lines, making it a valuable tool for studying ER-related signaling pathways and potential therapeutic applications in breast cancer research.
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SHIPPING AND STORAGE
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