ARV-825

Catalog No.S8297 Batch:S829702

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Technical Data

Formula

C46H47ClN8O9S
Molecular Weight 923.43 CAS No. 1818885-28-7
Solubility (25°C)* In vitro DMSO 100 mg/mL (108.29 mM)
Ethanol 6 mg/mL (6.49 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
7.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 150 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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.)

Preparing Stock Solutions

Biological Activity

Description ARV-825 is a BRD4 Inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 and sustained down-regulation of MYC.
Targets
BRD4 BD2 [1]
(Cell-free assay)		 BRD4 BD1 [1]
(Cell-free assay)
28 nM(Kd) 90 nM(Kd)
In vitro

Compared with the BRD4 inhibitors, ARV-825 treatment results in a strikingly more pronounced effect on the levels of c-MYC, and downstream cell proliferation and apoptosis induction in BL (Burkitt’s Lymphoma) cell lines[1].

The IC50s of ARV-825 for all tested cell lines and primary AML cells at 72 hours are in the low nanomolar range (2-50 nM). ARV-825 treatment reduces PIM1 levels and phosphorylation of CXCR4 in AML cells while overexpression of PIM1 or Myc reverses the phenomena[3].
In vivo

In a mouse model of human leukemia, the leukemia burdens are significantly lower in the ARV-825 treated mice as confirmed by luciferase imaging, flow cytometry, spleen size and survived longer compared to control mice[3].

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    RS4;11 cells

  • Concentrations

    3, 10, 30 nM

  • Incubation Time

    3 h

  • Method

    RS4;11 cells are treated for 3 h with each individual compound at indicated concentrations, and proteins are probed by specific antibodies.
Animal Study:

[4]
  • Animal Models

    NOD/SCID gamma mice

  • Dosages

    5 mg/kg

  • Administration

    i.p.

Selleck's ARV-825 has been cited by 7 publications

Dual Inhibition of CDK4/6 and XPO1 Induces Senescence With Acquired Vulnerability to CRBN-Based PROTAC Drugs [ Gastroenterology, 2024, S0016-5085(24)00062-3] PubMed: 38262581
Single-cell morphology encodes functional subtypes of senescence in aging human dermal fibroblasts [ bioRxiv, 2024, 2024.05.10.593637] PubMed: 38798365
Pharmacological inhibition of bromodomain and extra-terminal proteins induces an NRF-2-mediated antiviral state that is subverted by SARS-CoV-2 infection [ PLoS Pathog, 2023, 19(9):e1011657] PubMed: 37747932
FET fusion oncoproteins interact with BRD4 and SWI/SNF chromatin remodelling complex subtypes in sarcoma [ Mol Oncol, 2022, 10.1002/1878-0261.13195] PubMed: 35182012
Inhibition of BET Family Proteins Suppresses African Swine Fever Virus Infection [ Microbiol Spectr, 2022, 10(4):e0241921] PubMed: 35758684
Protein Ligand Interactions Using Surface Plasmon Resonance [ Methods Mol Biol, 2021, 2365:3-20] PubMed: 34432236
Activity of BET-proteolysis targeting chimeric (PROTAC) compounds in triple negative breast cancer. [ J Exp Clin Cancer Res, 2019, 38(1):383] PubMed: 31470872

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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.