2. Protein Tyrosine Kinase/RTK
  3. Btk
  4. Tolebrutinib

Tolebrutinib  (Synonyms: SAR442168; PRN2246)

Cat. No.: HY-109192 Purity: 99.12% ee.: 100.00%
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Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS).

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

CAS No. : 1971920-73-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 7 publication(s) in Google Scholar

Tolebrutinib Related Antibodies

Top Publications Citing Use of Products

    Tolebrutinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Sep 26;16(1):8477.  [Abstract]

    Quantification of MBP+ staining area, respectively (n = 3 MS hiPSC-lines; at least 30 glia-enriched organoids analyzed per experimental condition, respectively). The violin plots show the median (red line), quartiles (dotted lines), as well as the minima and maxima; each dot corresponds to one glia-enriched organoid. The results showed that Tolebrutinib (1 μM; 18 h) was able to rescue CSF-induced oligodendrocyte toxicity (MBP+ staining area ANOVA p < 0.0001).

    Tolebrutinib purchased from MedChemExpress. Usage Cited in: J Leukoc Biol. 2024 Jul 8:qiae160.  [Abstract]

    BTK inhibitors (evobrutinib, fenebrutinib, and Tolebrutinib) at concentrations of 1 µM or 10 µM or solvent control (0.01% DMSO). Afterward, neutrophils were activated with fMLF (1 nM) or CXCL8 (30 ng/mL) for 3 min. Cells were then fixed and microscopically scored as resting (round) or activated (blebbed/elongated) and the percentage activated cells of total cells was calculated. Next, the percentage inhibition of the treatments compared with DMSO control was calculated from the percentage activation.

    Tolebrutinib purchased from MedChemExpress. Usage Cited in: J Leukoc Biol. 2024 Jul 8:qiae160.  [Abstract]

    Purified neutrophils from healthy donors (n = 6) were treated with BTK inhibitors (evobrutinib, fenebrutinib, or Tolebrutinib) at concentrations of 0.1 µM, 1 µM, or 10 µM. Calcein AM (1 µM) and EthD-1 (0.5 µM) were added to visualize live and dead cells, respectively. DMSO (0.1%) and buffer were used as vehicle and negative control. The cells were imaged for 5 hours in the Incucyte imaging system and the percentage of dead cells (EthD-1+) was calculated.

    Tolebrutinib purchased from MedChemExpress. Usage Cited in: Immunohorizons. 2024 Sep 1;8(9):652-667.  [Abstract]

    Tolebrutinib (Tol, 1-10 μM). ICC images of p-BTK (red) and DAPI (blue) in human MDMs, mouse BMDMs, and microglia (scale bars, 100 μm).

    Tolebrutinib purchased from MedChemExpress. Usage Cited in: Immunohorizons. 2024 Sep 1;8(9):652-667.  [Abstract]

    Tolebrutinib (1-10 μM) significantly decreased p-BTK levels in human MDMs, mouse BMDMs, and primary mouse microglia (n = 6 per treatment per cell type). DMSO: 0.1% at 10 μM.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS)[1][2].

    IC50 & Target

    IC50: 0.7 nM (BTK; in HMC microglia cells)[2]
    In Vitro

    PRN2246 blocks the BCR-mediated activation (IC50=10 nM) and Fc receptor activation (IC50=166 and 9.6 nM for FcεR and FcγR, repectively) of immune cells[2].
    ? PRN2246 inhibits microglial FcγR activation through durable occupancy of BTK, with an IC50 of 157 nM[2].

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

    Tolebrutinib Related Antibodies
    In Vivo

    PRN2246 (1-5 mg/kg; p.o. q.d. for 28 d) produces dose-dependent protection from in myelin oligodendrocyte glycoprotein (MOG)-induced experimental autoimmune encephalomyelitis (EAE) model[2].

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

    455.51

    Formula

    C26H25N5O3
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O=C(N1[C@H]2CN(C(C=C)=O)CCC2)N(C3=CC=C(OC4=CC=CC=C4)C=C3)C5=C1C=CN=C5N
    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 : 87.5 mg/mL (192.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1953 mL 10.9767 mL 21.9534 mL
    5 mM 0.4391 mL 2.1953 mL 4.3907 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
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    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 (5.49 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 (5.49 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

    Purity: 99.12% ee.: 100.00%

    SDS (393 KB)

    COA (257 KB) HNMR (320 KB) RP-HPLC (259 KB) NP-HPLC (160 KB) LCMS (105 KB)

    Handling Instructions (2659 KB)
    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 2.1953 mL 10.9767 mL 21.9534 mL 54.8835 mL
    5 mM 0.4391 mL 2.1953 mL 4.3907 mL 10.9767 mL
    10 mM 0.2195 mL 1.0977 mL 2.1953 mL 5.4884 mL
    15 mM 0.1464 mL 0.7318 mL 1.4636 mL 3.6589 mL
    20 mM 0.1098 mL 0.5488 mL 1.0977 mL 2.7442 mL
    25 mM 0.0878 mL 0.4391 mL 0.8781 mL 2.1953 mL
    30 mM 0.0732 mL 0.3659 mL 0.7318 mL 1.8295 mL
    40 mM 0.0549 mL 0.2744 mL 0.5488 mL 1.3721 mL
    50 mM 0.0439 mL 0.2195 mL 0.4391 mL 1.0977 mL
    60 mM 0.0366 mL 0.1829 mL 0.3659 mL 0.9147 mL
    80 mM 0.0274 mL 0.1372 mL 0.2744 mL 0.6860 mL
    100 mM 0.0220 mL 0.1098 mL 0.2195 mL 0.5488 mL
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    Tolebrutinib 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:

    Tolebrutinib1971920-73-6SAR442168 PRN2246SAR 442168SAR-442168PRN2246PRN 2246PRN-2246BtkBruton tyrosine kinaseBrutontyrosinekinaseBTKmultiplesclerosisMSInhibitorinhibitorinhibit

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