Vepdegestrant-d5 (ARV-471-d5) is a deuterium-labeled derivative of Vepdegestrant, designed for stable isotope tracing in biochemical studies. It functions as a PROTAC (proteolysis-targeting chimera) to selectively degrade estrogen receptors, particularly in ER-positive breast cancer cells. By promoting the interaction between the estrogen receptor alpha and an intracellular E3 ligase complex, Vepdegestrant-d5 induces ubiquitylation and subsequent degradation of the receptor via the proteasome pathway. This compound exhibits significant biological activity, achieving a degradation concentration (DC50) of approximately 2 nM in relevant cell lines, making it a valuable tool for breast cancer research.
Vepdegestrant-d5 (ARV-471-d5) is a deuterium-labeled derivative of Vepdegestrant, designed for stable isotope tracing in biochemical studies. It functions as a PROTAC (proteolysis-targeting chimera) to selectively degrade estrogen receptors, particularly in ER-positive breast cancer cells. By promoting the interaction between the estrogen receptor alpha and an intracellular E3 ligase complex, Vepdegestrant-d5 induces ubiquitylation and subsequent degradation of the receptor via the proteasome pathway. This compound exhibits significant biological activity, achieving a degradation concentration (DC50) of approximately 2 nM in relevant cell lines, making it a valuable tool for breast cancer research.
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