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
More
Less

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
More
Less

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..…

More
Less

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

More
Less

ARV-471 Suppliers

Tianjin Lanshu Pharmaceutical Technology Co., Ltd
Tel
15210678165
Email
hanyachao@163.com
Country
China
ProdList
11
Advantage
58
Nantong Hi-Future Biotechnology Co., Ltd
Tel
18051384581
Email
sales@chemhifuture.com
Country
China
ProdList
2956
Advantage
58
Taizhou Nanfeng Pharmaceutical Research Institute
Tel
nanfengdrug@163.com; 18616377689
Email
nanfengdrug@163.com
Country
China
ProdList
20009
Advantage
58
Changzhou Borl Biotechnology Co.,LTD
Tel
13606124132;13656121842
Email
luyan0021@163.com
Country
China
ProdList
237
Advantage
58
Bayee Biotech (Anqing) Co., Ltd.
Tel
0556-5032306 18917961636
Email
wtx@bayeebio.com
Country
China
ProdList
208
Advantage
61
ChemFuture PharmaTech (Jiangsu) Ltd
Tel
5108538618
Fax
86 510 85386988-8017
Email
suger.wang@chemfuture.com
Country
China
ProdList
832
Advantage
65
WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
Tel
17702719238 18971495150;
Email
sales@sun-shinechem.com
Country
China
ProdList
1136
Advantage
64
Nanjing Chemlin Chemical Co., Ltd
Tel
13913916777
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
15984
Advantage
64
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185 18149758185;
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3505
Advantage
58
Shanghai Macklin Biochemical Co.,Ltd.
Tel
15221275939
Fax
021-50706099
Email
shenlinxing@macklin.cn
Country
China
ProdList
15801
Advantage
55

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
  • ARV-471, 10 mM in DMSO
  • ARV471 ,S9862
  • (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
  • 2229711-68-4
  • C45H49N5O4
  • t2z001