ARV-771

Product Name: ARV-771
CAS No.: 1949837-12-0
Chemical Name: ARV-771
Synonyms: ARV-771;ARV-771 ，S8532;ARV 771; ARV771;ARV-771, 10 mM in DMSO;Epigenetic Reader Domain,ARV-771,ARV771,inhibit,ARV 771,PROTACs,Inhibitor;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-;(2S,4R)-1-[(S)-2-(tert-Butyl)-15-[(S)-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-methyl-5-thiazolyl)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;(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

More

Less

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

More

Less

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.

More

Less

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

More

Less

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

More

Less

ARV-771 Suppliers

China 106 United States 6 USA 1 Global 113

Changzhou Borl Biotechnology Co.,LTD

Tel: 13606124132;13656121842
Email: luyan0021@163.com
Country: China
ProdList: 235
Advantage: 58

Beijing Ouhe Technology Co., Ltd

Tel: 010-010-82967028 13522913783
Fax: +86-10-82967029
Email: 2355560935@qq.com
Country: China
ProdList: 12000
Advantage: 60

Shanghai Topbiochem Technology Co., Ltd

Tel: 021-58170097
Email: info@topbiochem.com
Country: China
ProdList: 9510
Advantage: 58

SHANGHAI FORTUNE CHEMICAL TECHNOLOGY CO., LTD

Tel: 13816107857
Fax: qq: 276312098
Email: sales@fortunechem-sh.com
Country: China
ProdList: 984
Advantage: 58

Shanghai Macklin Biochemical Co.,Ltd.

Tel: 15221275939
Fax: 021-50706099
Email: shenlinxing@macklin.cn
Country: China
ProdList: 15873
Advantage: 55

Cool Pharm, Ltd

Tel: 021-60455363 18019463053
Fax: 50966098
Email: sales@coolpharm.com
Country: China
ProdList: 12346
Advantage: 58

Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
Fax: +86-21-52996696
Country: China
ProdList: 4757
Advantage: 55

ShangHai Angti Biotechnology Co., Ltd.

Tel: 13764913901
Fax: -
Email: info@angtibio.com
Country: China
ProdList: 4986
Advantage: 55

Shanghai YuanYe Biotechnology Co., Ltd.

Tel: 021-61312847; 18021002903
Fax: QQ:3008007432
Email: 3008007409@qq.com
Country: China
ProdList: 71826
Advantage: 60

ShangHai Biochempartner Co.,Ltd

Tel: 177-54423994 17754423994
Fax: QQ:2853530913
Email: 2853530910@QQ.com
Country: China
ProdList: 8000
Advantage: 62

More

Less

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:

ARV110 ARCC-4 ARV-825 ARV-471 Baloxavir marboxil BAM7 Auranofin Atopaxar Apixaban AMG 510 Baloxavir

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-[[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

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

ARV-771, 10 mM in DMSO

(2S,4R)-1-[(S)-2-(tert-Butyl)-15-[(S)-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-methyl-5-thiazolyl)phenyl]ethyl]pyrrolidine-2-carboxamide

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

ARV-771 ，S8532

1949837-12-0

C49H60ClN9O7S2

ADC LINKER

API