ARV-771

ChemicalBook > CAS DataBase List > ARV-771

Product Name: ARV-771
CAS No.: 1949837-12-0
Chemical Name: ARV-771
Synonyms: ARV-771;ARV 771; ARV771;Epigenetic Reader Domain,ARV-771,ARV771,inhibit,ARV 771,PROTACs,Inhibitor;(2S,4R)-1-[(2S)-2-[[2-[3-[2-[[2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetyl]amino]ethoxy]propoxy]acetyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-1,3-;(2S,4R)-1-((2S)-2-(tert-butyl)-15-((6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,14-dioxo-6,10-dioxa-3,13-diazapentadecan-1-oyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide;(2S,4R)-1-[(2S)-2-[[2-[3-[2-[[2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetyl]amino]ethoxy]propoxy]acetyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide
CBNumber: CB13167639
Molecular Formula: C49H60ClN9O7S2
Formula Weight: 986.65
MOL File: 1949837-12-0.mol

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ARV-771 Property

Density: 1.39±0.1 g/cm3(Predicted)
storage temp.: Sealed in dry,Store in freezer, under -20°C
solubility: DMSO:65.92(Max Conc. mg/mL);68.22(Max Conc. mM)
DMF:20.0(Max Conc. mg/mL);20.7(Max Conc. mM)
DMF:PBS (pH 7.2) (1:6):0.14(Max Conc. mg/mL);0.14(Max Conc. mM)
Ethanol:55.0(Max Conc. mg/mL);56.92(Max Conc. mM)
form: A crystalline solid
pka: 13.61±0.46(Predicted)
color: White to light yellow
InChIKey: PQOGZKGXGLHDGS-BZTQNJCZNA-N

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 21299
Product name: ARV-771
Packaging: 1mg
Price: $57
Updated: 2024/03/01

Cayman Chemical

Product number: 21299
Product name: ARV-771
Packaging: 10mg
Price: $253
Updated: 2024/03/01

Cayman Chemical

Product number: 21299
Product name: ARV-771
Packaging: 5mg
Price: $141
Updated: 2024/03/01

Tocris

Product number: 7256
Product name: ARV771
Purity: ≥98%(HPLC)
Packaging: 5
Price: $219
Updated: 2021/12/16

ChemScene

Product number: CS-6389
Product name: ARV-771
Purity: 99.82%
Packaging: 1mg
Price: $180
Updated: 2021/12/16

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ARV-771 Chemical Properties,Usage,Production

Description

ARV-771 is a BET PROTAC based on E3 ligase von Hippel-Lindau with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1) and BRD4(2), respectively.

Uses

ARV-771 is an effective BET degrader of the PROTAC class.

Biological Functions

ARV-771, a von Hippel–Landau (VHL) E3 ligase-based BET PROTAC, is highly active against cellular models of CRPC. ARV-771 in these cells results in rapid BET protein degradation with DC50 (the drug concentration that results in 50% protein degradation) values <1 nM. Interestingly, ARV–771–mediated BET degradation leads to decreased both FL-AR and AR-V7 at the transcript level. In contrast, treating CRPC cells with BET inhibitors leads to the suppression of AR-V7 but not of FL-AR levels. Moreover, ARV-771 causes significantly greater apoptotic cell death than a BET inhibitor. ARV-771 dramatically suppresses the proliferation of castration-resistant prostate cancer models via inducing Von Hippel Lindau (VHL) E3 ligase-mediated degradation of BRDs and inhibiting AR signaling. A subsequent study has demonstrated that ARV-771 can also suppress the proliferation of mantle cell lymphoma cells via increasing the levels of tumour suppressors, including CDKN1A/p21, HEXIM1, and NOXA[1].

Biological Activity

ARV-771 is a potent pan-(bromodomain and extra-terminal) BET degrader, a novel BET-PROTAC (proteolysis-targeting chimera), for BRD2(1), BRD2(2), BRD3(1) The Kd values of , BRD3(2), BRD4(1) and BRD4(2) were 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM and 7.6 nM, respectively.

target

td>

Target	Value
BRD2-BD2 (Cell-free assay)	4.7 nM(Kd)
BRD3-BD2 (Cell-free assay)	7.6 nM(Kd)
BRD4-BD2 (Cell-free assay)	7.6 nM(Kd)
BRD3-BD1 (Cell-free assay)	8.3 nM(Kd)
BRD4-BD1 (Cell-free assay)	9.6 nM(Kd)

storage

Store at -20°C

References

[1] Yuanfei Deng. “ARV-771 Acts as an Inducer of Cell Cycle Arrest and Apoptosis to Suppress Hepatocellular Carcinoma Progression.” Frontiers in Pharmacology (2022).

ARV-771 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from ARV-771 manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD

Product: ARV-771 1949837-12-0
Price: US $0.00/mg
Min. Order: 1mg
Purity: 98%min
Supply Ability: 500mg
Release date: 2021-08-26

Hubei Chuchang Biotech Co., Ltd.

Product: ARV-771 1949837-12-0
Price: US $0.00-0.00/MG
Min. Order: 1MG
Purity: 98
Supply Ability: 100G
Release date: 2024-04-17

1949837-12-0, ARV-771Related Search:

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ARV-771

ARV 771; ARV771

(2S,4R)-1-[(2S)-2-[[2-[3-[2-[[2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetyl]amino]ethoxy]propoxy]acetyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide

(2S,4R)-1-((2S)-2-(tert-butyl)-15-((6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,14-dioxo-6,10-dioxa-3,13-diazapentadecan-1-oyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

Epigenetic Reader Domain,ARV-771,ARV771,inhibit,ARV 771,PROTACs,Inhibitor

1949837-12-0

C49H60ClN9O7S2

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