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
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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P501Dispose of contents/container to..…
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
ARV-471 Suppliers
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