ChemicalBook > CAS DataBase List > ARV-471
ARV-471
- Product Name
- ARV-471
- CAS No.
- 2229711-68-4
- Chemical Name
- ARV-471
- Synonyms
- ARV-471;ARV471 ，S9862;Vepdegestrant;Vepdegestrant（ARV-471）;ARV-471, 10 mM in DMSO;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;(3S)-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]-2,6-piperidinedione;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)
- pka
- 10.36±0.60(Predicted)
- form
- Solid
- color
- White to off-white
- InChIKey
- TZZDVPMABRWKIZ-XMOGEVODSA-N
- SMILES
- N1C(=O)CC[C@H](N2CC3=C(C2=O)C=CC(N2CCN(CC4CCN(C5=CC=C([C@@H]6C7=C(C=C(O)C=C7)CC[C@@H]6C6=CC=CC=C6)C=C5)CC4)CC2)=C3)C1=O
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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.
in vivo
Vepdegestrant (3-30 mpk, p.o, daily) inhibits tumor growth in estradiol-dependent MCF7 xenografts and reduces tumor ER protein[2].
ARV-471 Preparation Products And Raw materials
Raw materials
Preparation Products
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