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Vepdegestrant (ARV-471) is an oral estrogen receptor PROTAC protein degrader for breast cancer. Vepdegestrant (ARV-471) is a heterobifunctional molecule that promotes the interaction between estrogen receptor alpha and intracellular E3 ligase complexes. Vepdegestrant (ARV-471) causes ubiquitination and subsequent degradation of the estrogen receptor via the proteasome. Vepdegestrant (ARV-471) potently degrades ER-positive The ER in breast cancer cell lines is potently degraded by ARV-471 with a DC50 value of approximately 2 nM.
Molecular Weight | 723.9 |
Formula | C45H49N5O4 |
CAS Number | 2229711-68-4 |
Solubility (25°C) | DMSO 90 mg/mL |
Storage | -20°C, protect from light, dry, sealed |
[2] Diego Garcia Jimenez, et al. ADMET DMPK. Are we ready to design oral PROTACs®?
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