2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. ARV-825

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.

For research use only. We do not sell to patients.

ARV-825 Chemical Structure

ARV-825 Chemical Structure

CAS No. : 1818885-28-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 280 In-stock
Solution
10 mM * 1 mL in DMSO USD 280 In-stock
Solid
1 mg USD 72 In-stock
5 mg USD 180 In-stock
10 mg USD 220 In-stock
50 mg USD 450 In-stock
100 mg USD 750 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 22 publication(s) in Google Scholar

ARV-825 Related Antibodies

Top Publications Citing Use of Products

    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.

    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: 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.

    View All PROTACs Isoform Specific Products:

    View All Isoforms
    von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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.

    IC50 & Target

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

    ARV-825 Related Antibodies
    Molecular Weight

    923.43

    Formula

    C46H47ClN8O9S
    CAS No.
    Appearance

    Solid

    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    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.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.0829 mL 5.4146 mL 10.8292 mL
    5 mM 0.2166 mL 1.0829 mL 2.1658 mL
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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.

    • 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.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • 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

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: 99.32%

    COA (248 KB) LCMS (108 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

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

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

    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
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    ARV-825 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    ARV-8251818885-28-7ARV825ARV 825PROTACsEpigenetic Reader DomainInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Salutation

    Applicant Name *

    		 

    Email Address *

    Phone Number *

    		 

    Organization Name *

    Department *

    		 

    Requested quantity *

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    ARV-825
    Cat. No.:
    HY-16954
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.