Art. -Nr.: HY-16954

ARV-825

37 Cited Publications

Kundenbewertung

Based on 37 publication(s) in Google Scholar

ARV-825 is a PROTAC connected by ligands for Cereblon and BRD4. ARV-825 binds to BD1 and BD2 of BRD4 with K_ds of 90 and 28 nM, respectively.

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Reinheit: 99.21%
CAS. Nr.: 1818885-28-7
Formel: C₄₆H₄₇ClN₈O₉S
Molecular Weight:923.43

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

ARV-825 Chemical Structure

CAS. Nr.: 1818885-28-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (37)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

ARV-825 is a PROTAC connected by ligands for Cereblon and BRD4. ARV-825 binds to BD1 and BD2 of BRD4 with K_ds of 90 and 28 nM, respectively.

IC₅₀ & Target

Kd: 90 nM (Bromodomain 1 of BRD4), 28 nM (Bromodomain 2 of BRD4)^[1]

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CA46	DC₅₀	<1 nM Compound: 21; ARV-825	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 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	[PMID: 31047748]
MOLM-13	IC₅₀	18.2 nM Compound: 6; ARV-825	Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28339196]
MOLM-13	IC₅₀	18.2 nM Compound: ARV-825	Growth inhibition of human MOLM13 cells after 96 hrs by CCK8 assay Growth inhibition of human MOLM13 cells after 96 hrs by CCK8 assay	[PMID: 30019901]
MV4-11	IC₅₀	1.05 nM Compound: ARV-825	Growth inhibition of human MV4-11 cells after 96 hrs by CCK8 assay Growth inhibition of human MV4-11 cells after 96 hrs by CCK8 assay	[PMID: 30019901]
RS4-11	IC₅₀	3.3 nM Compound: 6; ARV-825	Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28339196]
RS4-11	IC₅₀	3.3 nM Compound: ARV-825	Growth inhibition of human RS4:11 cells after 96 hrs by CCK8 assay Growth inhibition of human RS4:11 cells after 96 hrs by CCK8 assay	[PMID: 30019901]

In Vitro

ARV-825 is a hetero-bifunctional proteolysis-targeting chimera (PROTAC) that recruits BRD4 to the E3 ubiquitin ligase cereblon. ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of the former via the proteasome. Given that BRD4 and cereblon binding moieties in ARV-825 have K_ds of 28-90 nM and ~3 μM to their respective targets, this suggests that ARV-825 acts in a substoichiometric way in mediating BRD4 degradation. ARV-825 treatment results in prolonged BRD4 down-regulation and downstream signaling suppression compared to BRD4 inhibitors^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1818885-28-7
Appearance Solid
Molecular Weight 923.43
Formel C₄₆H₄₇ClN₈O₉S
Color Light yellow to yellow
SMILES

CC1=NN=C2N1C(SC(C)=C3C)=C3C(C4=CC=C(Cl)C=C4)=N[C@H]2CC(NC5=CC=C(OCCOCCOCCOCCNC6=C(C(N(C7CCC(NC7=O)=O)C8=O)=O)C8=CC=C6)C=C5)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (37)

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Journal Impact Factor

Nat Aging

Comparative analysis of senolytic drugs reveals mitochondrial determinants of efficacy and resistance. [Abstract]

2026 Feb;6(2):316-328. PMID: 41611832
Nat Aging

SARS-CoV-2 infection triggers paracrine senescence and leads to a sustained senescence-associated inflammatory response. [Abstract]

2022 Feb;2(2):115-124. PMID: 37117754
Nat Commun

Hepatocyte growth factor derived from senescent cells attenuates cell competition-induced apical elimination of oncogenic cells. [Abstract]

2022 Jul 18;13(1):4157. PMID: 35851277
Nat Commun

A proximity biotinylation-based approach to identify protein-E3 ligase interactions induced by PROTACs and molecular glues. [Abstract]

2022 Jan 10;13(1):183. PMID: 35013300
Nat Commun

BRD4 prevents the accumulation of R-loops and protects against transcription-replication collision events and DNA damage. [Abstract]

2020 Aug 14;11(1):4083. PMID: 32796829

ARV-825 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Aug 14;11(1):4083. [Abstract]

Representative IF images and quantification of nuclear S9.6 intensity, γH2AX foci, and RNase H1 in HeLa cells in the absence (−DOX) or presence (+DOX) of doxycycline-induced FLAG-tagged RNase H1 expression for 24 h, followed by treatment with 100 nM ARV-825 for 6 h.

ARV-825 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Aug 14;11(1):4083. [Abstract]

Cells treated with ARV-825 shows marked degradation of BRD4 protein and significantly reduces levels of MYC protein, demonstrating reduced levels of BRD4-driven MYC transcription.
Nat Commun

A BET family protein degrader provokes senolysis by targeting NHEJ and autophagy in senescent cells. [Abstract]

2020 Apr 22;11(1):1935. PMID: 32321921
Acta Pharm Sin B

2026 May 19.
J Adv Res

Redistribution of super-enhancers promotes malignancy in human hepatocellular carcinoma. [Abstract]

2025 Jul 4:S2090-1232(25)00504-1. PMID: 40617410
Biomaterials

Tumor microenvironment responsive nano-PROTAC for BRD4 degradation enhanced cancer photo-immunotherapy. [Abstract]

2025 May 7:322:123387. PMID: 40344878
Mater Today Bio

A pH-responsive PROTAC-based nanosystem triggers tumor-specific ferroptosis to construct in situ tumor vaccines. [Abstract]

2025 Jan 24:31:101523. PMID: 39935894
Clin Cancer Res

Overcoming BET Inhibitor Resistance in Malignant Peripheral Nerve Sheath Tumors. [Abstract]

2019 Jun 1;25(11):3404-3416. PMID: 30796033
Cell Commun Signal

Inhibition of bromodomain and extra-terminal proteins targets constitutively active NFκB and STAT signaling in lymphoma and influences the expression of the antiapoptotic proteins BCL2A1 and c-MYC. [Abstract]

2024 Aug 27;22(1):415. PMID: 39192247
Cell Commun Signal

BRD4/nuclear PD-L1/RelB circuit is involved in the stemness of breast cancer cells. [Abstract]

2023 Nov 3;21(1):315. PMID: 37924094
J Med Chem

Alkyne Two-Phase Strategy: Rapid Generation of TK-285-Derived PROTACs as BRD4 Degraders. [Abstract]

2026 Mar 19. PMID: 41852276
Anal Chem

Hydrogen/Deuterium Exchange for Chiral Stability Assessment in Acidic Methine-Containing Compounds. [Abstract]

2025 Dec 2;97(47):26097-26107. PMID: 41243541
JCI Insight

Inhibition of bromodomain extraterminal histone readers alleviates skin fibrosis in experimental models of scleroderma. [Abstract]

2022 May 9;7(9):e150871. PMID: 35349485
Biochem Pharmacol

Discovery of a potent BRD4 PROTAC and evaluation of its bioactivity in breast cancer cell lines. [Abstract]

2025 Jul 12:241:117159. PMID: 40659131
Mol Cancer Ther

Harnessing senolytics and PARP inhibition to expand the antitumor activity of CDK4/6 inhibitors in prostate cancer. [Abstract]

2025 Jul 2. PMID: 40601842
Int J Mol Sci

BRD4 Mediates Transforming Growth Factor-β-Induced Smooth Muscle Cell Differentiation from Mesenchymal Progenitor Cells. [Abstract]

2025 Aug 21;26(16):8074. PMID: 40869394
Cancers (Basel)

BRD4 Inhibition as a Strategy to Prolong the Response to Standard of Care in Estrogen Receptor-Positive Breast Cancer. [Abstract]

2023 Aug 11;15(16):4066. PMID: 37627092
Cancer Sci

MYC Addiction as a Targetable Vulnerability in Nelarabine-Resistant T-Cell Acute Lymphoblastic Leukemia. [Abstract]

2026 Jun;117(6):1608-1622. PMID: 41947770
Structure

PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]

2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062
J Cell Mol Med

Inactivation of CDK12 Enhances Mitochondrial Efficiency to Suppress DNA Damage. [Abstract]

2026 Apr;30(7):e71101. PMID: 41896195
Hum Gene Ther

HIV Tat- conjugated Histone H3 peptides induce tumor cell death via cellular stress responses. [Abstract]

2023 Jan;34(1-2):42-55. PMID: 36373826
J Biol Chem

Degradation and inhibition of epigenetic regulatory protein BRD4 exacerbate Alzheimer's disease-related neuropathology in cell models. [Abstract]

2022 Apr;298(4):101794. PMID: 35248531
Aging

ARV-825-induced BRD4 protein degradation as a therapy for thyroid carcinoma. [Abstract]

2020 Mar 12;12(5):4547-4557. PMID: 32163373
Sci Rep

Interplay between interferon regulatory factor 1 and BRD4 in the regulation of PD-L1 in pancreatic stellate cells. [Abstract]

2018 Sep 5;8(1):13225. PMID: 30185888

ARV-825 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Sep 5;8(1):13225. [Abstract]

ARV-825 decreases IFN-γ-induced PD-L1 mRNA and protein expression in primary PSCs and in the stellate cell line.
Environ Toxicol

Transcriptional factor BRD4 promotes the stemness of esophageal cancer by activating the nuclear PD-L1/RelB axis. [Abstract]

2024 Feb;39(2):669-679. PMID: 37615218
J Pharm Biomed Anal

Development and optimization of a high-throughput LC-MS/MS method for the simultaneous determination of Exatecan and its Cathepsin B-sensitive prodrug, and ARV-825 in rat plasma: Application to pharmacokinetic study. [Abstract]

2025 Jun 15:258:116746. PMID: 39955884
Invest New Drugs

Targeting Myc through BET-PROTAC elicits potent anti-lymphoma activity in diffuse large B cell lymphoma. [Abstract]

2025 Jun;43(3):621-633. PMID: 40307411
bioRxiv

2025 Sep 7.
Indiana University Indianapolis

2025.
bioRxiv

2025 April 30.
bioRxiv

2024 Mar 21.
University of Texas

2023 Jun 13.
Research Square Print

November 18th, 2022
Martin-Luther-Universität Halle-Wittenberg

2020 Dec.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 50 mg/mL (54.15 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.0829 mL

5.4146 mL

10.8292 mL

5 mM

0.2166 mL

1.0829 mL

2.1658 mL

10 mM

0.1083 mL

0.5415 mL

1.0829 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (2.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (2.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

Affinity of compounds (e.g., ARV-825) with Bromodomain 1 and 2 of BRD4 is determined with BROMOscan by DiscoverX^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.0829 mL	5.4146 mL	10.8292 mL	27.0730 mL
	5 mM	0.2166 mL	1.0829 mL	2.1658 mL	5.4146 mL
	10 mM	0.1083 mL	0.5415 mL	1.0829 mL	2.7073 mL
	15 mM	0.0722 mL	0.3610 mL	0.7219 mL	1.8049 mL
	20 mM	0.0541 mL	0.2707 mL	0.5415 mL	1.3536 mL
	25 mM	0.0433 mL	0.2166 mL	0.4332 mL	1.0829 mL
	30 mM	0.0361 mL	0.1805 mL	0.3610 mL	0.9024 mL
	40 mM	0.0271 mL	0.1354 mL	0.2707 mL	0.6768 mL
	50 mM	0.0217 mL	0.1083 mL	0.2166 mL	0.5415 mL

Keywords

ARV-825

37 Cited Publications

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ARV-825

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

PROTAC Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) ARV-825

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (37)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ARV-825

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

PROTAC Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) ARV-825

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (37)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ARV-825 Related Classifications

HY-16954 Related Classifications