Vepdegestrant (ARV-471), an ER-targeting protein degrader for breast cancer, is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex, leading to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. ARV-471 robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of ~ 1 nM. PROTAC-mediated ER degradation decreases the expression of classically-regulated ER-target genes and inhibits cell proliferationof ER-dependent cell lines (MCF7, T47D).
MedKoo Cat#: 207154
Name: Vepdegestrant
CAS#: 2229711-08-2
Chemical Formula: C45H49N5O4
Exact Mass: 723.3785
Molecular Weight: 723.92
Elemental Analysis: C, 74.66; H, 6.82; N, 9.67; O, 8.84
The following data is based on the product molecular weight 723.92 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
