2. Protein Tyrosine Kinase/RTK Autophagy
  3. c-Met/HGFR Autophagy
  4. Tepotinib

Tepotinib  (Synonyms: EMD-1214063)

Cat. No.: HY-14721 Purity: 99.87%
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Tepotinib (EMD-1214063) is a potent and highly selective c-Met inhibitor with an IC50 of 4 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Antitumor effects.

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

Tepotinib Chemical Structure

Tepotinib Chemical Structure

CAS No. : 1100598-32-0

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Solid + Solvent
10 mM * 1 mL in DMSO
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 USD 103 In-stock
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10 mM * 1 mL in DMSO USD 103 In-stock
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10 mg USD 150 In-stock
50 mg USD 480 In-stock
100 mg USD 690 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Tepotinib Related Antibodies

Top Publications Citing Use of Products

    Tepotinib purchased from MedChemExpress. Usage Cited in: Gene Expr. 2018 May 18;18(2):135-147.  [Abstract]

    Western blot for Myc-tag shows decrease in Myc-tag levels at 8 weeks of EMD1214063 treatment only. GAPDH shows comparable loading in all lanes.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Tepotinib (EMD-1214063) is a potent and highly selective c-Met inhibitor with an IC50 of 4 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Antitumor effects[1].

    In Vitro

    Tepotinib (EMD 1214063) inhibits IRAK4, TrkA, Axl, IRAK1, Mer, and TrkA with IC50s of 615, 1017, 1566, 2037, 2272, and 5716 nM, respectively[1].
    Exposure of A549 cells to EMD 1214063 results in inhibition of HGF-induced c-Met phosphorylation, with an average IC50 of 6 nM[1].
    EMD 1214063 (0.01 nM-30 μM) inhibits tumor cell proliferation and migration in vitro[1].

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

    Tepotinib Related Antibodies

    Cell Viability Assay[1]

    Cell Line: MKN-45 gastric cancer cells
    Concentration: 0.01 nM, 0.03 nM, 0.1 nM, 0.3 nM, 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1 μM, 3 μM, 10 μM and 30 μM
    Incubation Time: 72 hours
    Result: Considerably inhibited the viability of MKN-45 cells with IC50 values of less than 1 nM.
    In Vivo

    Tepotinib (EMD 1214063) induces tumor regression in xenograft models[1].
    Tepotinib inhibit in vivo c-Met phosphorylation[1].

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

    Animal Model: CD-1 or BALB/C nude mice bearing human cancer cell lines KP-4, or EBC-1[1]
    Dosage: 6 and 15 mg/kg for mice bearing NSCLC EBC-1; 25, 50 and 200 mg/kg for mice bearing pancreatic carcinoma cell line KP-4.
    Administration: Injected daily; for 14-18 days
    Result: Daily administration of 5 or 15 mg/kg to EBC-1 tumor-bearing mice resulted in effective inhibition or complete tumor regression, respectively.
    Induced dose-dependent tumor growth inhibition in mice bearing human pancreatic carcinoma KP-4 tumors.
    Molecular Weight

    492.57

    Formula

    C29H28N6O2
    CAS No.
    Appearance

    Solid

    SMILES

    N#CC1=CC=CC(C(C=CC2=O)=NN2CC3=CC=CC(C4=NC=C(C=N4)OCC5CCN(CC5)C)=C3)=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 : 11.11 mg/mL (22.56 mM; ultrasonic and warming and heat to 60°C; 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 2.0302 mL 10.1508 mL 20.3017 mL
    5 mM 0.4060 mL 2.0302 mL 4.0603 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.

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    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Volume
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    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: ≥ 0.62 mg/mL (1.26 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.62 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 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: ≥ 0.62 mg/mL (1.26 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.62 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 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: 99.87%

    COA (243 KB) LCMS (123 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 2.0302 mL 10.1508 mL 20.3017 mL 50.7542 mL
    5 mM 0.4060 mL 2.0302 mL 4.0603 mL 10.1508 mL
    10 mM 0.2030 mL 1.0151 mL 2.0302 mL 5.0754 mL
    15 mM 0.1353 mL 0.6767 mL 1.3534 mL 3.3836 mL
    20 mM 0.1015 mL 0.5075 mL 1.0151 mL 2.5377 mL
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    Tepotinib 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:

    Tepotinib1100598-32-0EMD-1214063EMD1214063EMD 1214063c-Met/HGFRAutophagyInhibitorinhibitorinhibit

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