2. Protein Tyrosine Kinase/RTK Apoptosis
  3. VEGFR c-Met/HGFR c-Kit TAM Receptor FLT3 Apoptosis
  4. Cabozantinib

Cabozantinib  (Synonyms: XL184; BMS-907351)

Cat. No.: HY-13016 Purity: 99.96%
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Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis.

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

Cabozantinib Chemical Structure

Cabozantinib Chemical Structure

CAS No. : 849217-68-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 44 publication(s) in Google Scholar

Other Forms of Cabozantinib:

Cabozantinib Related Antibodies

Top Publications Citing Use of Products

40 Publications Citing Use of MCE Cabozantinib

WB

    Cabozantinib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2017 Nov;16(11):2387-2398.  [Abstract]

    Representative Western blots and densitometry show that cabozantinib reduces phosphorylation of Erk1/2 after 6 hours and reduces cyclin D1 and increases p27 protein levels after 24 hours of treatment (n=3-4).

    Cabozantinib purchased from MedChemExpress. Usage Cited in: PLoS One. 2017 Sep 25;12(9):e0185321.  [Abstract]

    Treatment with Cabozantinib results in complete inhibition of the c-MET phosphorylation stimulated by HGF at nanomolar concentrations.

    Cabozantinib purchased from MedChemExpress. Usage Cited in: J Med Chem. 2016 Jan 14;59(1):358-73.  [Abstract]

    Autophosphorylation of RET and its downstream signaling are blocked by 6i. The effect of 6i on autophosphorylation of RET in (A) RET-WT Ba/F3, (B) RET-S891A Ba/F3, (C) RET-V804L Ba/F3 and (D) RET-V804M Ba/F3. (A-D) Ba/F3 cells, stably transformed with the indicated constructs, are treated for 1 h with gradually increasing concentrations of 7a, Cabozantinib and 6i (0-10 μM) and then lysed. Protein extracts are immunoblotted with antibodies specific for the Y905 and Y1062 phosphorylated forms of R

    Cabozantinib purchased from MedChemExpress. Usage Cited in: J Med Chem. 2016 Jan 14;59(1):358-73.  [Abstract]

    Autophosphorylation of RET and its downstream signaling are blocked by 6i. The effect of 6i on autophosphorylation of RET in (A) RET-WT Ba/F3, (B) RET-S891A Ba/F3, (C) RET-V804L Ba/F3 and (D) RET-V804M Ba/F3. (A-D) Ba/F3 cells, stably transformed with the indicated constructs, are treated for 1 h with gradually increasing concentrations of 7a, Cabozantinib and 6i (0-10 μM) and then lysed. Protein extracts are immunoblotted with antibodies specific for the Y905 and Y1062 phosphorylated forms of R

    View All VEGFR Isoform Specific Products:

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    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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    Axl Mer Tyro3

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis[1][2].

    IC50 & Target[1]

    VEGFR2

    0.035 nM (IC50)

    Axl

     

    Flt-4

    6 nM (IC50)

    Flt-1

    12 nM (IC50)

    Met

    1.3 ± 1.2 nM (IC50)

    In Vitro

    Cabozantinib inhibits phosphorylation of MET and VEGFR2, as well as KIT, FLT3, and AXL with IC50 values of 7.8, 1.9, 5.0, 7.5, and 42 μM, respectively[1].
    Cabozantinib (4.6 nM) inhibits tubule formation with no evidence of cytotoxicity, with IC50 values of 6.7, 5.1, 4.1, 7.7, and 4.7 nM in HMVEC, MDA-MB-231, A431, HT1080, and B16F10 cells, respectively[1].
    Cabozantinib (0-370 nM, 24 h) inhibits cellular migration and invasion[1].
    Cabozantinib (48 h) inhibits tumor cell proliferation in a variety of tumor types[1].

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

    Cabozantinib Related Antibodies

    Cell Proliferation Assay

    Cell Line: SNU-5, Hs746T, SNU-1, SNU-16, MDA-MB-231, U87MG, H441, H69, and PC3 cells[1]
    Concentration:
    Incubation Time: 48 hours
    Result: Inhibited tumor cell proliferation, with IC50 of 19, 9.9, 5223, 1149, 6421, 1851, 21700, 20200, and 10800 nM, respectively.

    Cell Migration Assay

    Cell Line: B16F10 cells[1]
    Concentration: 0, 41, 123, and 370 nM
    Incubation Time: 24 hours
    Result: Potently inhibited HGF-induced migration (IC50 = 31 nM) of B16F10 cells.

    Cell Invasion Assay

    Cell Line: B16F10 cells[1]
    Concentration: 0, 1.5, 14, and 123 nM
    Incubation Time: 24 hours
    Result: Potently inhibited HGF-induced invasion (IC50 = 9 nM) of B16F10 cells.
    In Vivo

    Cabozantinib (100 mg/kg, Orally, once) inhibits MET and VEGFR2 phosphorylation in mice[1].
    Cabozantinib (100 mg/kg, Orally, once) significantly increases tumor hypoxia and apoptosis[1].
    Cabozantinib (0-60 mg/kg, Orally, once daily for 14 days) inhibits tumor growth in a dose-dependent manner[1].

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

    Animal Model: Female mice bearing MBA-MB-231 tumor (5 per group)[1]
    Dosage: 0, 100 mg/kg
    Administration: Orally, once
    Result: Inhibited MET and VEGFR2 phosphorylation.
    Animal Model: Mice bearing MBA-MB-231 tumor[1]
    Dosage: 1, 3, 10, 30, 60 mg/kg
    Administration: Orally, once daily for 14 days
    Result: Inhibited tumor growth in a dose-dependent manner.
    Clinical Trial
    Molecular Weight

    501.51

    Formula

    C28H24FN3O5
    CAS No.
    Appearance

    Solid

    Color

    White to gray

    SMILES

    O=C(C1(CC1)C(NC2=CC=C(F)C=C2)=O)NC3=CC=C(C=C3)OC4=C5C=C(OC)C(OC)=CC5=NC=C4
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light

    *In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (49.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 1 mg/mL (1.99 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9940 mL 9.9699 mL 19.9398 mL
    5 mM 0.3988 mL 1.9940 mL 3.9880 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 (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Concentration
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    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:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.98 mM); Clear solution

    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.15 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

    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:  0.5% CMC/saline water

      Solubility: 2.5 mg/mL (4.98 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).

    *In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

    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%

    COA (251 KB) LCMS (110 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, 2 years; -20°C, 1 year (protect from light). 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
    H2O / DMSO 1 mM 1.9940 mL 9.9699 mL 19.9398 mL 49.8495 mL
    DMSO 5 mM 0.3988 mL 1.9940 mL 3.9880 mL 9.9699 mL
    10 mM 0.1994 mL 0.9970 mL 1.9940 mL 4.9849 mL
    15 mM 0.1329 mL 0.6647 mL 1.3293 mL 3.3233 mL
    20 mM 0.0997 mL 0.4985 mL 0.9970 mL 2.4925 mL
    25 mM 0.0798 mL 0.3988 mL 0.7976 mL 1.9940 mL
    30 mM 0.0665 mL 0.3323 mL 0.6647 mL 1.6616 mL
    40 mM 0.0498 mL 0.2492 mL 0.4985 mL 1.2462 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Cabozantinib 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:

    Cabozantinib849217-68-1XL184 BMS-907351XL 184XL-184BMS907351BMS 907351BMS-907351VEGFRc-Met/HGFRc-KitTAM ReceptorFLT3ApoptosisVascular endothelial growth factor receptorSCFRCD117Tyro3AxlMerCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3angiogenesisantiangiogenicapoptosisMBA-MB-231B16F10 cellsA431HT1080Inhibitorinhibitorinhibit

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