ARV-771

Catalog No.S8532

For research use only.

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

CAS No. 1949837-12-0

Selleck's ARV-771 has been cited by 1 Publication

Purity & Quality Control

Choose Selective PROTAC Inhibitors

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

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]

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]

Protocol (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • Animal Models: Mice implanted subcutaneously with 5 × 106 22Rv1 or VCaP cells
  • Dosages: 30 mg/kg
  • Administration: IH/SC

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 986.64
Formula

C49H60ClN9O7S2

CAS No. 1949837-12-0
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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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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