1. Protein Tyrosine Kinase/RTK
  2. Itk
  3. BMS-509744

BMS-509744 is a potent, selective and ATP competitive Itk inhibitor with an IC50 of 19 nM.

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

BMS-509744 Chemical Structure

BMS-509744 Chemical Structure

CAS No. : 439575-02-7

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 158 In-stock
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10 mM * 1 mL in DMSO USD 158 In-stock
Solid
5 mg USD 115 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    BMS-509744 purchased from MedChemExpress. Usage Cited in: Cancer Cell Int. 2019 Feb 14;19:32.  [Abstract]

    Cells are treated with indicated concentrations of BMS-509744 for 24 h, then whole cell lysates are detected by western blot for phosphorylated FAK and total RhoA.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    BMS-509744 is a potent, selective and ATP competitive Itk inhibitor with an IC50 of 19 nM.

    IC50 & Target

    IC50: 19 nM (Itk)[1]

    In Vitro

    BMS-509744 reduces T-cell receptor-induced functions including PLCγ1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion, and T-cell proliferation in vitro in both human and mouse cells. BMS-488516 and BMS-509744 potently inhibit Itk in vitro with IC50 values of 96 and 19 nM, respectively. Both compounds exhibit competitive kinetics with respect to ATP, suggesting that they bind to the ATP binding site of the Itk kinase domain[1].

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

    In Vivo

    BMS-509744 and BMS-488516 suppress the production of IL-2 induced by anti-T-cell receptor antibody administered to mice. BMS-509744 exhibits a 50% inhibitory capacity when dosed at 50 mg/kg, irrespective of the amount of induction antibody. BMS-509744 also significantly diminishes lung inflammation in a mouse model of ovalbumin-induced allergy/asthma[1].

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

    Molecular Weight

    623.83

    Formula

    C32H41N5O4S2

    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    CC(C(C)(C)C)NCC1=CC=C(C(NC2=NC=C(SC3=CC(C(N4CCN(C(C)=O)CC4)=O)=C(OC)C=C3C)S2)=O)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 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 21.9 mg/mL (35.11 mM; Need ultrasonic and warming; 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 1.6030 mL 8.0150 mL 16.0300 mL
    5 mM 0.3206 mL 1.6030 mL 3.2060 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 (4.01 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 (4.01 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: 98.09%

    References
    Kinase Assay
    [1]

    BMS-509744 activity (IC50) is determined by kinase assays. The kinase reactions are performed in the presence of 10 μM GST-SLP-76 and various concentrations of ATP for 10 min using 10 ng of enzyme. The concentrations of BMS-509744

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

    Animal Administration
    [1]

    Mice: Balb/c mice are injected subcutaneously with the compounds (BMS-509744 and BMS-488516) or vehicle (H2O:ethanol:Tween 80 ) 90:5:5) 15 min before intravenous administration of anti-CD3 antibody. Serum is collected for the analysis of IL-2 and compound levels at 90 min after anti-CD3 antibody administration. IL-2 is measured by ELISA, and compound levels are measured by mass spectrometry[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 1.6030 mL 8.0150 mL 16.0300 mL 40.0750 mL
    5 mM 0.3206 mL 1.6030 mL 3.2060 mL 8.0150 mL
    10 mM 0.1603 mL 0.8015 mL 1.6030 mL 4.0075 mL
    15 mM 0.1069 mL 0.5343 mL 1.0687 mL 2.6717 mL
    20 mM 0.0802 mL 0.4008 mL 0.8015 mL 2.0038 mL
    25 mM 0.0641 mL 0.3206 mL 0.6412 mL 1.6030 mL
    30 mM 0.0534 mL 0.2672 mL 0.5343 mL 1.3358 mL
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    BMS-509744 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:
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    Cat. No.:
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