ARV-825
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 Kds of 90 and 28 nM, respectively.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.21%
- CAS 番号: 1818885-28-7
- 分子式: C46H47ClN8O9S
- 分子量:923.43
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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MedChemExpress（MCE）の使用を引用している文献 ARV-825
More- Nat Aging. 2026 Feb;6(2):316-328. [Abstract]
- Nat Aging. 2022 Feb;2(2):115-124. [Abstract]
- Nat Commun. 2022 Jul 18;13(1):4157. [Abstract]
- Nat Commun. 2022 Jan 10;13(1):183. [Abstract]
- Nat Commun. 2020 Aug 14;11(1):4083. [Abstract]
- Nat Commun. 2020 Apr 22;11(1):1935. [Abstract]
- J Adv Res. 2025 Jul 4:S2090-1232(25)00504-1. [Abstract]
- Acta Pharm Sin B. 2026 May 19.
- Biomaterials. 2025 May 7:322:123387. [Abstract]
- Cell Commun Signal. 2024 Aug 27;22(1):415. [Abstract]
- Cell Commun Signal. 2023 Nov 3;21(1):315. [Abstract]
- Mater Today Bio. 2025 Jan 24:31:101523. [Abstract]
- Clin Cancer Res. 2019 Jun 1;25(11):3404-3416. [Abstract]
- J Med Chem. 2026 Mar 19. [Abstract]
- Anal Chem. 2025 Dec 2;97(47):26097-26107. [Abstract]
- Mol Cancer Ther. 2025 Jul 2. [Abstract]
- JCI Insight. 2022 May 9;7(9):e150871. [Abstract]
- Biochem Pharmacol. 2025 Jul 12:241:117159. [Abstract]
- Int J Mol Sci. 2025 Aug 21;26(16):8074. [Abstract]
- Cancer Sci. 2026 Jun;117(6):1608-1622. [Abstract]
- Sci Rep. 2018 Sep 5;8(1):13225. [Abstract]
- Cancers (Basel). 2023 Aug 11;15(16):4066. [Abstract]
- J Cell Mol Med. 2026 Apr;30(7):e71101. [Abstract]
- Structure. 2024 Dec 5;32(12):2352-2363.e8. [Abstract]
- Hum Gene Ther. 2023 Jan;34(1-2):42-55. [Abstract]
- J Biol Chem. 2022 Apr;298(4):101794. [Abstract]
- Invest New Drugs. 2025 Jun;43(3):621-633. [Abstract]
- J Pharm Biomed Anal. 2025 Jun 15:258:116746. [Abstract]
- bioRxiv. 2025 Sep 7.
- Indiana University Indianapolis. 2025.
- bioRxiv. 2025 April 30.
- bioRxiv. 2024 Mar 21.
- Environ Toxicol. 2024 Feb;39(2):669-679. [Abstract]
- University of Texas. 2023 Jun 13.
- Research Square Print. November 18th, 2022
- Martin-Luther-Universität Halle-Wittenberg. 2020 Dec.
- Aging. 2020 Mar 12;12(5):4547-4557. [Abstract]
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生物活性
Kd: 90 nM (Bromodomain 1 of BRD4), 28 nM (Bromodomain 2 of BRD4)[1]
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Cell Line
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Type | Value | Description | References |
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| CA46 | DC50 |
<1 nM
Compound: 21; ARV-825
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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
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[PMID: 31047748] |
| MOLM-13 | IC50 |
18.2 nM
Compound: 6; ARV-825
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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
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[PMID: 28339196] |
| MOLM-13 | IC50 |
18.2 nM
Compound: ARV-825
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Growth inhibition of human MOLM13 cells after 96 hrs by CCK8 assay
Growth inhibition of human MOLM13 cells after 96 hrs by CCK8 assay
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[PMID: 30019901] |
| MV4-11 | IC50 |
1.05 nM
Compound: ARV-825
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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
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[PMID: 30019901] |
| RS4-11 | IC50 |
3.3 nM
Compound: 6; ARV-825
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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
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[PMID: 28339196] |
| RS4-11 | IC50 |
3.3 nM
Compound: ARV-825
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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
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[PMID: 30019901] |
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 Kds 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.
化学情報
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CAS 番号 1818885-28-7
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性状 Solid
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分子量 923.43
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分子式 C46H47ClN8O9S
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Color Light yellow to yellow
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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
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
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Most Recent
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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.
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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 -
J Adv Res
2025 Jul 4:S2090-1232(25)00504-1. PMID: 40617410 -
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Biomaterials
Tumor microenvironment responsive nano-PROTAC for BRD4 degradation enhanced cancer photo-immunotherapy. [Abstract]2025 May 7:322:123387. PMID: 40344878 -
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
2023 Nov 3;21(1):315. PMID: 37924094 -
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
2019 Jun 1;25(11):3404-3416. PMID: 30796033 -
J Med Chem
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 -
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 -
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 -
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 -
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 -
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.
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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 -
J Cell Mol Med
2026 Apr;30(7):e71101. PMID: 41896195 -
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 -
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 -
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 -
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 -
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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 -
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Aging
2020 Mar 12;12(5):4547-4557. PMID: 32163373
溶剤 & 溶解度
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.
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
純度とドキュメンテーション
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データシート (274 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
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.
| 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 |
ARV-825 関連分類
HY-16954 関連分類
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