ChemicalBook > CAS DataBase List > ARV-471

ARV-471

Product Name
ARV-471
CAS No.
2229711-68-4
Chemical Name
ARV-471
Synonyms
ARV-471;Vepdegestrant;Vepdegestrant(ARV-471);3-(4-hydroxy-6-methyl-1-oxoisoindolin-2-yl)piperidine-2,6-dione;(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;oral,Inhibitor,breast cancer,PROTAC,E3 ligase,inhibit,hetero-bifunctional,ubiquitylation,ARV-471,PROTACs,Estrogen Receptor/ERR,ARV 471,estrogen receptor,ARV471,proteasome;2,6-Piperidinedione, 3-[1,3-dihydro-1-oxo-5-[4-[[1-[4-[(1R,2S)-1,2,3,4-tetrahydro-6-hydroxy-2-phenyl-1-naphthalenyl]phenyl]-4-piperidinyl]methyl]-1-piperazinyl]-2H-isoindol-2-yl]-, (3S)-
CBNumber
CB48816045
Molecular Formula
C45H49N5O4
Formula Weight
723.9
MOL File
2229711-68-4.mol
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ARV-471 Property

Density 
1.275±0.06 g/cm3(Predicted)
solubility 
DMSO : 110 mg/mL (151.95 mM; Need ultrasonic)
form 
Solid
pka
10.36±0.60(Predicted)
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

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ARV-471 Chemical Properties,Usage,Production

Uses

ARV-471 is a best-in-class, orally active estrogen receptor (ER) PROTAC degrader. It is developed for the research of breast cancer.

Biological Activity

ARV-471 is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. It leads 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 ~2 nM.

ARV-471 Preparation Products And Raw materials

Raw materials

Preparation Products

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2229711-68-4, ARV-471Related Search:


  • 2,6-Piperidinedione, 3-[1,3-dihydro-1-oxo-5-[4-[[1-[4-[(1R,2S)-1,2,3,4-tetrahydro-6-hydroxy-2-phenyl-1-naphthalenyl]phenyl]-4-piperidinyl]methyl]-1-piperazinyl]-2H-isoindol-2-yl]-, (3S)-
  • ARV-471
  • Vepdegestrant
  • Vepdegestrant(ARV-471)
  • (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
  • oral,Inhibitor,breast cancer,PROTAC,E3 ligase,inhibit,hetero-bifunctional,ubiquitylation,ARV-471,PROTACs,Estrogen Receptor/ERR,ARV 471,estrogen receptor,ARV471,proteasome
  • 3-(4-hydroxy-6-methyl-1-oxoisoindolin-2-yl)piperidine-2,6-dione
  • 2229711-68-4
  • C45H49N5O4
  • t2z001