(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.
(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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