2. Protein Tyrosine Kinase/RTK
  3. TAM Receptor
  4. UNC2250

UNC2250 is a potent and selective Mer inhibitor with an IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3.

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

UNC2250 Chemical Structure

UNC2250 Chemical Structure

CAS No. : 1493694-70-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

UNC2250 Related Antibodies

Top Publications Citing Use of Products

    UNC2250 purchased from MedChemExpress. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278.  [Abstract]

    BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM) with the indicated antagonist of TAM receptor (LDC1267 at 1 µM, UNC2250 at 5 µM, R428 at 5 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 12 h.

    View All TAM Receptor Isoform Specific Products:

    View All Isoforms
    Axl Mer Tyro3

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    UNC2250 is a potent and selective Mer inhibitor with an IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3.

    IC50 & Target

    Axl

     

    Mer

     

    In Vitro

    UNC2250 (5-500 nM; 1 hour) inhibits Mer phosphorylation in 697 B-ALL cells with an IC50 value of 9.8 nM[1].
    UNC2250 efficiently inhibits ligand-dependent phosphorylation of a chimeric protein consisting of the extracellular and transmembrane domains of the epidermal growth factor (EGF) receptor and the intracellular tyrosine kinase domain of Mer[1].
    UNC2250 incubation inhibits colony formation in soft agar cultures of the BT-12 rhabdoid tumor and the Colo699 NSCLC cell lines[1] .

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

    UNC2250 Related Antibodies

    Western Blot Analysis[1]

    Cell Line: 697 B-ALL cells
    Concentration: 5, 10, 20, 50, 100, 250, 500 nM
    Incubation Time: 1 hour
    Result: Inhibits Mer phosphorylation in 697 B-ALL cells with an IC50 value of 9.8 nM.
    Molecular Weight

    440.58

    Formula

    C24H36N6O2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    CCCCNC1=NC(N[C@@H]2CC[C@@H](O)CC2)=C(C3=CC=C(CN4CCOCC4)C=N3)C=N1
    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: 

    0.1 M HCL : 12.5 mg/mL (28.37 mM; ultrasonic and adjust pH to 3 with HCl)

    DMSO : ≥ 10 mg/mL (22.70 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 2.2697 mL 11.3487 mL 22.6974 mL
    5 mM 0.4539 mL 2.2697 mL 4.5395 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
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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    90% Corn Oil

      Solubility: ≥ 2 mg/mL (4.54 mM); Clear solution

      This protocol yields a clear solution of ≥ 2 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 (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    • Protocol 2

      Add each solvent one by one:  10% DMSO    20% HS-15    70% Saline

      Solubility: ≥ 1 mg/mL (2.27 mM); Clear solution

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (22.70 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 10 mg/mL (22.70 mM); Suspended solution; Need ultrasonic

    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
    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 / 0.1 M HCL 1 mM 2.2697 mL 11.3487 mL 22.6974 mL 56.7434 mL
    5 mM 0.4539 mL 2.2697 mL 4.5395 mL 11.3487 mL
    10 mM 0.2270 mL 1.1349 mL 2.2697 mL 5.6743 mL
    15 mM 0.1513 mL 0.7566 mL 1.5132 mL 3.7829 mL
    20 mM 0.1135 mL 0.5674 mL 1.1349 mL 2.8372 mL
    0.1 M HCL 25 mM 0.0908 mL 0.4539 mL 0.9079 mL 2.2697 mL
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    UNC2250 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:

    UNC22501493694-70-4UNC 2250UNC-2250TAM ReceptorTyro3AxlMerInhibitorinhibitorinhibit

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