Home Others PROTAC chemical ARV-771 For research use only.

ARV-771

ARV-771 is a potent pan-(bromodomain and extra-terminal)BET degrader, a novel BET-PROTAC(proteolysis-targeting chimera) with Kd 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.

ARV-771 Chemical Structure

ARV-771 Chemical Structure

CAS No. 1949837-12-0

Purity & Quality Control

ARV-771 Related Products

Biological Activity

Description ARV-771 is a potent pan-(bromodomain and extra-terminal)BET degrader, a novel BET-PROTAC(proteolysis-targeting chimera) with Kd 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.
Targets
BRD2-BD2 [1]
(Cell-free assay)		 BRD3-BD2 [1]
(Cell-free assay)		 BRD4-BD2 [1]
(Cell-free assay)		 BRD3-BD1 [1]
(Cell-free assay)		 BRD4-BD1 [1]
(Cell-free assay)		 Click to View More Targets
4.7 nM(Kd) 7.6 nM(Kd) 7.6 nM(Kd) 8.3 nM(Kd) 9.6 nM(Kd)
In vitro
In vitro

ARV-771 is a potent small-molecule pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved efficacy in cellular models of CRPC as compared with BET inhibition. ARV-771 treatment of CRPC cells results in apoptosis.[1]
Cell Research Cell lines 22Rv1 cells, VCaP cells, LnCaP95 cells
Concentrations 1-300 nM
Incubation Time 24 h, 72 h
Method

c-MYC ELISA. 22Rv1 cells (30,000 cells per well) were dosed with ARV-771 serially diluted at 1:3 ratio for an eight-point dose curve. AR ELISA. VCaP cells (40,000 cells per well) were dosed with ARV-771 serially diluted at 1:3 ratio for an eight-point dose curve. Cell Proliferation Assay Protocol. 22Rv1 cells (5,000 cells per well) were dosed with ARV-771 serially diluted 1:3 for a 10-point dose curve for 72 h.
In Vivo
In vivo

ARV-771 induces degradation in vivo. ARV-771 results in suppression of both AR signaling and AR levels and leads to tumor regression in a CRPC mouse xenograft model.[1]
Animal Research Animal Models Mice implanted subcutaneously with 5 × 106 22Rv1 or VCaP cells
Dosages 30 mg/kg
Administration IH/SC

Chemical Information & Solubility

Molecular Weight 986.64 Formula

C49H60ClN9O7S2
CAS No. 1949837-12-0 SDF --
Smiles CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)NCCOCCCOCC(=O)NC(C(=O)N4CC(CC4C(=O)NC(C)C5=CC=C(C=C5)C6=C(N=CS6)C)O)C(C)(C)C)C7=CC=C(C=C7)Cl)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (101.35 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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