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Chemical Structure : ARV-471
CAS No.: 2229711-68-4
Catalog No.: PC-72621Not For Human Use, Lab Use Only.
ARV-471 (Vepdegestrant) is an investigational orally bioavailable PROTAC protein degrader designed to specifically target and degrade the estrogen receptor (ER) with DC50 of 1.8 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 1 mg | $198 | In stock | |
| 5 mg | $458 | In stock | |
| 10 mg | $758 | In stock | |
| 25 mg | Get quote |
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ARV-471 (Vepdegestrant) is an investigational orally bioavailable PROTAC protein degrader designed to specifically target and degrade the estrogen receptor (ER) with DC50 of 1.8 nM.
ARV-471 induces ER degradation in multiple ER+ breast cancer cell lines, including MCF-7 cells and ESR1-mutant lines, shows potential as both a single agent and in combination with CDK4/6 inhibitors, as well as superior inhibition of tumor growth compared to Fulvestrant.
| M.Wt | 723.379 | |
| Formula | C45H49N5O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
100 mM in DMSO (72.3 mg/mL) |
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| Chemical Name/SMILES |
(S)-3-(5-(4-((1-(4-((1R,2S)-6-hydroxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenyl)piperidin-4-yl)methyl)piperazin-1-yl)-1-oxoisoindolin-2-yl)piperidine-2,6-dione |
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1. Lin X, et al. Eur J Med Chem. 2020 Nov 15;206:112689.
2. Wang C, et al. Eur J Med Chem. 2021 Dec 5;225:113749.
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