ARV-771

Catalog No.S8532 Batch:S853202

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Technical Data

Formula

C49H60ClN9O7S2
Molecular Weight 986.64 CAS No. 1949837-12-0
Solubility (25°C)* In vitro DMSO 100 mg/mL (101.35 mM)
Ethanol 100 mg/mL (101.35 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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)		 View More
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 Assay:

[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 Study:

[1]
  • Animal Models

    Mice implanted subcutaneously with 5 × 106 22Rv1 or VCaP cells

  • Dosages

    30 mg/kg

  • Administration

    IH/SC

Selleck's ARV-771 has been cited by 2 publications

Targeting of vulnerabilities of drug-tolerant persisters identified through functional genetics delays tumor relapse [ Cell Rep Med, 2024, 5(3):101471] PubMed: 38508142
ARV-771 Acts as an Inducer of Cell Cycle Arrest and Apoptosis to Suppress Hepatocellular Carcinoma Progression [ Front Pharmacol, 2022, 13:858901] PubMed: 35600879

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.