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

BMS-509744 

Cat. No.: HY-11092 Purity: 97.05%
Handling Instructions

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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 214 In-stock
Estimated Time of Arrival: December 31
5 mg USD 156 In-stock
Estimated Time of Arrival: December 31
10 mg USD 240 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1080 In-stock
Estimated Time of Arrival: December 31
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200 mg   Get quote  

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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    BMS-509744 purchased from MCE. Usage Cited in: Cancer Cell Int. 2019 Feb 14;19:32.

    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].

    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].

    Molecular Weight

    623.83

    Formula

    C₃₂H₄₁N₅O₄S₂

    CAS No.

    439575-02-7

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 21.9 mg/mL (35.11 mM; Need ultrasonic and warming)

    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
    10 mM 0.1603 mL 0.8015 mL 1.6030 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    *All of the co-solvents are provided by MCE.
    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

    Purity: 97.05%

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    Keywords:

    BMS-509744BMS509744BMS 509744ItkInterleukin-2 inducible T-cell kinaseIL2 inducible T-cell kinaseInhibitorinhibitorinhibit

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    Product name:
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    Cat. No.:
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