Home Epigenetics PROTAC chemical - Epigenetic Reader Domain inhibitor ARV-825 For research use only.

ARV-825

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.

ARV-825 Chemical Structure

ARV-825 Chemical Structure

CAS No. 1818885-28-7

Purity & Quality Control

ARV-825 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
22RV1 Function assay 24 hrs Induction of CRBN-mediated BRD4 degradation in human 22RV1 cells measured after 24 hrs by immunoblotting analysis, DC50 = 0.00057 μM. 30684871
NAMALWA Function assay overnight Protac activity at Cereblon/BRD4 in human NAMALWA cells assessed as induction of BRD4 protein degradation in human NAMALWA cells after overnight incubation by immunoblot method, DC50 = 0.001 μM. 31047748
CA46 Function assay overnight Protac activity at Cereblon/BRD4 in human CA46 cells assessed as induction of BRD4 protein degradation in human CA46 cells after overnight incubation by immunoblot analysis, DC50 = 0.001 μM. 31047748
MV4-11 Growth inhibition assay 96 hrs Growth inhibition of human MV4-11 cells after 96 hrs by CCK8 assay, IC50 = 0.00105 μM. 30019901
RS4:11 Cytotoxicity assay 4 days Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay, IC50 = 0.0033 μM. 28339196
RS4:11 Growth inhibition assay 96 hrs Growth inhibition of human RS4:11 cells after 96 hrs by CCK8 assay, IC50 = 0.0033 μM. 30019901
MV4-11 Antiproliferative assay 48 hrs Antiproliferative activity against human MV4-11 cells after 48 hrs by CellTiter-Glo luminescent cell viability assay, EC50 = 0.01698 μM. 28595007
MOLM13 Cytotoxicity assay 4 days Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay, IC50 = 0.0182 μM. 28339196
MOLM13 Growth inhibition assay 96 hrs Growth inhibition of human MOLM13 cells after 96 hrs by CCK8 assay, IC50 = 0.0182 μM. 30019901
HL60 Antiproliferative assay 48 hrs Antiproliferative activity against human HL60 cells after 48 hrs by CellTiter-Glo luminescent cell viability assay, EC50 = 0.03467 μM. 28595007
RS4:11 Function assay 3 to 30 nM 3 hrs Induction of cereblon/cullin 4A-mediated BRD2 degradation in human RS4:11 cells at 3 to 30 nM after 3 hrs by Western blot method 28339196
RS4:11 Function assay 3 to 30 nM 3 hrs Induction of cereblon/cullin 4A-mediated BRD3 degradation in human RS4:11 cells at 3 to 30 nM after 3 hrs by Western blot method 28339196
RS4:11 Function assay 3 to 30 nM 3 hrs Induction of cereblon/cullin 4A-mediated BRD4 degradation in human RS4:11 cells at 3 to 30 nM after 3 hrs by Western blot method 28339196
U266 Function assay 12 hrs Induction of CRBN-mediated BRD4 degradation in human U266 cells up to 1000 nM measured after 12 hrs by immunoblotting analysis 30684871
U266 Function assay 12 hrs Induction of CRBN ubiquitin ligase-mediated IKZF1 degradation in human U266 cells up to 1000 nM measured after 12 hrs by immunoblotting analysis 30684871
Click to View More Cell Line Experimental Data

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
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].
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot BRD1 / BRD2 / BRD3 / BRD4 / p21 c-MYC PARP / cleaved PARP CDK6 / CDK4 cleaved caspase 9 / cleaved caspase 3 Akt / pAKT-S473 / mTOR / p-mTOR-S2448 / p70S6K / p70S6K-T389 / 4EBP1/ p-4EBP1-S65 / PDK1 / p-PDK1-S241 / PI3K / p-PI3K-T458 JAK2 / p-STAT5 / p-STAT3 / PIM1 / p27 / Bcl-xl / γH2AX 30903020
Immunofluorescence BRD4 28042144
Growth inhibition assay Cell viability 26051217
In Vivo
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].
Animal Research Animal Models NOD/SCID gamma mice
Dosages 5 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 923.43 Formula

C46H47ClN8O9S
CAS No. 1818885-28-7 SDF --
Smiles CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)NC4=CC=C(C=C4)OCCOCCOCCOCCNC5=CC=CC6=C5C(=O)N(C6=O)C7CCC(=O)NC7=O)C8=CC=C(C=C8)Cl)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (108.29 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble


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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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