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ARV-471

Chemical Structure : ARV-471

CAS No.: 2229711-68-4

ARV-471 (Vepdegestrant, ARV471)

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 723.379
Formula C45H49N5O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

100 mM in DMSO (72.3 mg/mL)

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

References

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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