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
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
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.
N-Bromosuccinimide Price
- Product number
- 21299
- Product name
- ARV-771
- Packaging
- 1mg
- Price
- $57
- Updated
- 2024/03/01
- Product number
- 21299
- Product name
- ARV-771
- Packaging
- 10mg
- Price
- $253
- Updated
- 2024/03/01
- Product number
- 21299
- Product name
- ARV-771
- Packaging
- 5mg
- Price
- $141
- Updated
- 2024/03/01
- Product number
- 7256
- Product name
- ARV771
- Purity
- ≥98%(HPLC)
- Packaging
- 5
- Price
- $219
- Updated
- 2021/12/16
- Product number
- CS-6389
- Product name
- ARV-771
- Purity
- 99.82%
- Packaging
- 1mg
- Price
- $180
- Updated
- 2021/12/16
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
| Target | Value |
| BRD2-BD2 (Cell-free assay) | 4.7 nM(Kd) |
| BRD3-BD2 (Cell-free assay) | 7.6 nM(Kd) | td>
| 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
ARV-771 Suppliers
View Lastest Price from ARV-771 manufacturers
- 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
- 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