1. Protein Tyrosine Kinase/RTK
  2. Src
  3. Src Inhibitor 1

Src Inhibitor 1  (Synonyms: Src Kinase Inhibitor 1; Src-l1)

Cat. No.: HY-101053 Purity: 99.96%
COA Handling Instructions

Src Inhibitor 1 is a potent, ATP-competitive and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.

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

Src Inhibitor 1 Chemical Structure

Src Inhibitor 1 Chemical Structure

CAS No. : 179248-59-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 69 In-stock
Solution
10 mM * 1 mL in DMSO USD 69 In-stock
Solid
2 mg USD 60 In-stock
5 mg USD 84 In-stock
10 mg USD 114 In-stock
25 mg USD 264 In-stock
50 mg USD 474 In-stock
100 mg   Get quote  
200 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 10 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Src Inhibitor 1 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. December 2022, 109340.

    SRC inhibitor 1 (5 μM) significantly reduces SRC phosphorylation in the mouse chondrocytes.

    View All Src Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Src Inhibitor 1 is a potent, ATP-competitive and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.

    IC50 & Target

    IC50: 44 nM (Src), 88 nM (Lck)[1]

    In Vitro

    Src Inhibitor 1 is competitive with both ATP and peptide binding sites of the kinase. The IC50 values are 44 and 88 nM for Src and Lck, respectively[1]. Src Inhibitor 1 is found to be a potent inhibitor of Src (IC50=0.18 μM), but also inhibited other Src family members, such as Lck, Csk and Yes with similar potency to Src, and RIP2 (IC50=0.026 μM) with even greater potency. In addition, it inhibited CHK2 with similar potency to Src, and Aurora B with slightly lower potency[2].

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

    Molecular Weight

    373.40

    Formula

    C22H19N3O3

    CAS No.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    COC1=CC2=NC=NC(NC3=CC=C(OC4=CC=CC=C4)C=C3)=C2C=C1OC

    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 : 9.09 mg/mL (24.34 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 2.6781 mL 13.3905 mL 26.7809 mL
    5 mM 0.5356 mL 2.6781 mL 5.3562 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    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 0.91 mg/mL (2.44 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.91 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (9.1 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 0.91 mg/mL (2.44 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.91 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 (9.1 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: 99.96%

    References
    Kinase Assay
    [2]

    Assays (25.5 μL volume) are carried out robotically at room temperature (21°C) and are linear with respect to time and enzyme concentration under the conditions used. Assays are performed for 30 min using Multidrop Micro reagent dispensers in a 96-well format. The concentration of magnesium acetate in the assays is 10 mM and [γ-33P]ATP (800 c.p.m./pmol) is used at 5, 20 or 50 μM as indicated, in order to be at or below the Kmfor ATP for each enzyme.The assays are initiated with MgATP, stopped by the addition of 5 μL of 0.5 M orthophosphoric acid and spotted on to P81 filter plates using a unifilter harvester. The IC50 values of inhibitors are determined after carrying out assays at ten different concentrations of each compound[2].

    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 2.6781 mL 13.3905 mL 26.7809 mL 66.9523 mL
    5 mM 0.5356 mL 2.6781 mL 5.3562 mL 13.3905 mL
    10 mM 0.2678 mL 1.3390 mL 2.6781 mL 6.6952 mL
    15 mM 0.1785 mL 0.8927 mL 1.7854 mL 4.4635 mL
    20 mM 0.1339 mL 0.6695 mL 1.3390 mL 3.3476 mL
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    Src Inhibitor 1 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:
    Src Inhibitor 1
    Cat. No.:
    HY-101053
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