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| | ARV-471 Basic information |
| Product Name: | ARV-471 | | Synonyms: | 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 | | CAS: | 2229711-68-4 | | MF: | C45H49N5O4 | | MW: | 723.9 | | EINECS: | | | Product Categories: | t2z001 | | Mol File: | 2229711-68-4.mol |  |
| | ARV-471 Chemical Properties |
| 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 |
| | ARV-471 Usage And Synthesis |
| 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 |
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