1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. Spebrutinib

Spebrutinib  (Synonyms: AVL-292; CC-292)

Cat. No.: HY-18012 Purity: 99.62%
COA Handling Instructions

Spebrutinib (AVL-292; CC-292) is a covalent, orally active, and highly selective with an IC50 of 0.5 nM.

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

Spebrutinib Chemical Structure

Spebrutinib Chemical Structure

CAS No. : 1202757-89-8

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Solid + Solvent
10 mM * 1 mL in DMSO
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USD 73 In-stock
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10 mM * 1 mL in DMSO USD 73 In-stock
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10 mg USD 99 In-stock
50 mg USD 165 In-stock
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Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of Spebrutinib:

Top Publications Citing Use of Products

    Spebrutinib purchased from MedChemExpress. Usage Cited in: Blood. 2016 Jun 23;127(25):3237-52.  [Abstract]

    Ibrutinib binds to the ATP-binding pocketof HCK and blocks ATP binding. Results from kinase active-site inhibition assaysutilizing an ATP-BTN probe that is used to pull downactive kinases in the presence of Ibrutinib, CC-292, or A419259 in lysates from BCWM.1 WM cells.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Spebrutinib (AVL-292; CC-292) is a covalent, orally active, and highly selective with an IC50 of 0.5 nM.

    IC50 & Target

    IC50: <0.5 nM (Btk)[1]

    In Vitro

    Spebrutinib (CC-292) is a covalent, highly selective, orally active inhibitor of Btk with IC50 value of 0.5 nM. Spebrutinib also less potently inhibits Yes, c-Src, Brk, Lyn, and Fyn with IC50s of 723 nM, 1.729 μM, 2.43 μM, 4.4 μM, and 7.15 μM, rspectively. Extensive analysis has revealed that the EC50 of Btk occupancy from a Spebrutinib dose-response in Ramos cells (EC50=6 nM) correlated directly with the cellular EC50 of Btk kinase inhibition with Spebrutinib (EC50=8 nM). Furthermore, the concentration at which Spebrutinib inhibits 90% of Btk activity in Ramos cells is 35 nM while the concentration of Spebrutinib required for 90% occupancy of Btk is 39 nM[1].

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

    Clinical Trial
    Molecular Weight

    423.44

    Formula

    C22H22FN5O3

    CAS No.
    Appearance

    Solid

    Color

    White to khaki

    SMILES

    COCCOC1=CC=C(NC2=NC=C(F)C(NC3=CC=CC(NC(C=C)=O)=C3)=N2)C=C1

    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    DMSO : ≥ 45 mg/mL (106.27 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 2.3616 mL 11.8080 mL 23.6161 mL
    5 mM 0.4723 mL 2.3616 mL 4.7232 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • 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 (5.90 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 (5.90 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: 99.62%

    References
    Cell Assay
    [1]

    Cells are incubated in serum-free RPMI media for 1-1.5 hours. Isolated human B cells are incubated with Spebrutinib at a final concentration of 0.001, 0.01, 0.1 and 1 μM. Ramos cells are incubated with 0.1 nM-3 μM Spebrutinib. Cells are then incubated in the presence of compound for 1 hour at 37°C. Following incubation, cells are centrifuged and resuspended in 100 μL of serum-free RPMI and BCR is stimulated with addition of 5 μg/mL α-human IgM. Samples are centrifuged, washed in phosphate-buffered saline (PBS), and lysed in 100 μL of Cell Extraction Buffer plus 1:10 (v/v) PhosSTOP Phosphatase Inhibitor and 1:10 (v/v) Complete Protease Inhibitor. Antibodies used for immunoblot analysis include P-PLCγ2, PLCγ2 (3871; CST), Syk (2712; CST), P-Syk (2710; CST), Btk, P-Btk, and Tubulin. Membranes are scanned on a Li-Cor Odyssey scanner using infrared fluorescence detection[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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3616 mL 11.8080 mL 23.6161 mL 59.0402 mL
    5 mM 0.4723 mL 2.3616 mL 4.7232 mL 11.8080 mL
    10 mM 0.2362 mL 1.1808 mL 2.3616 mL 5.9040 mL
    15 mM 0.1574 mL 0.7872 mL 1.5744 mL 3.9360 mL
    20 mM 0.1181 mL 0.5904 mL 1.1808 mL 2.9520 mL
    25 mM 0.0945 mL 0.4723 mL 0.9446 mL 2.3616 mL
    30 mM 0.0787 mL 0.3936 mL 0.7872 mL 1.9680 mL
    40 mM 0.0590 mL 0.2952 mL 0.5904 mL 1.4760 mL
    50 mM 0.0472 mL 0.2362 mL 0.4723 mL 1.1808 mL
    60 mM 0.0394 mL 0.1968 mL 0.3936 mL 0.9840 mL
    80 mM 0.0295 mL 0.1476 mL 0.2952 mL 0.7380 mL
    100 mM 0.0236 mL 0.1181 mL 0.2362 mL 0.5904 mL
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    Spebrutinib 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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