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  2. Epigenetic Reader Domain Apoptosis
  3. Mivebresib

Mivebresib  (Synonyms: ABBV-075)

Cat. No.: HY-100015 Purity: 99.42%
COA Handling Instructions

Mivebresib (ABBV-075) est un inhibiteur puissant et oralement actif de bromodomaine et un bromodomaine du domaine extraterminal (BET). Mivebresib se lie à BRD4 avec un Ki de 1,5 nM.

Mivebresib (ABBV-075) ist ein potenter und oral aktiver Inhibitor der bromodomain and extraterminal domain (BET) bromodomain. Mivebresib bindet an BRD4 mit einem Ki von 1.5 nM.

Mivebresib (ABBV-075) is a potent and orally active bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a Ki of 1.5 nM.

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

Mivebresib Chemical Structure

Mivebresib Chemical Structure

CAS No. : 1445993-26-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 133 In-stock
Solution
10 mM * 1 mL in DMSO USD 133 In-stock
Solid
2 mg USD 106 In-stock
5 mg USD 132 In-stock
10 mg USD 198 In-stock
25 mg USD 330 In-stock
50 mg USD 594 In-stock
100 mg USD 990 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 8 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Mivebresib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 Jul 19;10(8):557.   [Abstract]

    BET inhibitors reduce IDO1 transcription.The protein levels of IDO1 are determined by RT-qPCR and western blotting, respectively.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Mivebresib (ABBV-075) is a potent and orally active bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a Ki of 1.5 nM[1].

    IC50 & Target

    IC50: 1.5 nM (BRD4)[1]

    In Vitro

    Mivebresib inhibit DHT-stimulated transcription of AR target genes without significant effect on AR protein expression. In addition to blocking the transcription activation downstream of AR, Mivebresib is also a potent inhibitor of MYC and the TMPRSS2-ETS fusion proteins[1].

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

    Clinical Trial
    Molecular Weight

    459.47

    Formula

    C22H19F2N3O4S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CCS(=O)(NC1=CC=C(OC2=CC=C(F)C=C2F)C(C3=CN(C)C(C4=C3C=CN4)=O)=C1)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (217.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1764 mL 10.8821 mL 21.7642 mL
    5 mM 0.4353 mL 2.1764 mL 4.3528 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • 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 (5.44 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.44 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    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
    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1764 mL 10.8821 mL 21.7642 mL 54.4105 mL
    5 mM 0.4353 mL 2.1764 mL 4.3528 mL 10.8821 mL
    10 mM 0.2176 mL 1.0882 mL 2.1764 mL 5.4411 mL
    15 mM 0.1451 mL 0.7255 mL 1.4509 mL 3.6274 mL
    20 mM 0.1088 mL 0.5441 mL 1.0882 mL 2.7205 mL
    25 mM 0.0871 mL 0.4353 mL 0.8706 mL 2.1764 mL
    30 mM 0.0725 mL 0.3627 mL 0.7255 mL 1.8137 mL
    40 mM 0.0544 mL 0.2721 mL 0.5441 mL 1.3603 mL
    50 mM 0.0435 mL 0.2176 mL 0.4353 mL 1.0882 mL
    60 mM 0.0363 mL 0.1814 mL 0.3627 mL 0.9068 mL
    80 mM 0.0272 mL 0.1360 mL 0.2721 mL 0.6801 mL
    100 mM 0.0218 mL 0.1088 mL 0.2176 mL 0.5441 mL
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    Mivebresib 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.

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    Product Name:
    Mivebresib
    Cat. No.:
    HY-100015
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