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

Cabozantinib  (Synonyms: XL184; BMS-907351)

Cat. No.: HY-13016 Purity: 99.96%
COA Handling Instructions

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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Customer Review

Based on 35 publication(s) in Google Scholar

Other Forms of Cabozantinib:

Top Publications Citing Use of Products

31 Publications Citing Use of MCE Cabozantinib

WB

    Cabozantinib purchased from MCE. 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 MCE. 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 MCE. 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 MCE. 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).

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    • Biological Activity

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    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)

    Flt-4

    6 nM (IC50)

    Flt-1

    12 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].

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

    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].

    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.
    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, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (49.85 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

    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
    10 mM 0.1994 mL 0.9970 mL 1.9940 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  30% polypropylene glycol, 5% Tween-80 and 65% D5W (dextrose 5% water)

      Solubility: 10 mg/mL (19.94 mM); Suspended solution; Need ultrasonic

    • 2.

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

      Solubility: 2.5 mg/mL (4.98 mM); Suspended solution; Need ultrasonic

    • 3.

      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

    • 4.

      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

    • 5.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.08 mg/mL (4.15 mM); Suspended solution; Need ultrasonic

    • 6.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.96%

    References
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    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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    Cat. No.:
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