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

Cabozantinib hydrochloride  (Synonyms: XL184 hydrochloride; BMS-907351 hydrochloride)

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

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CAS No. : 1817759-42-4

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Cabozantinib hydrochloride Related Antibodies

Top Publications Citing Use of Products

56 Publications Citing Use of MCE Cabozantinib hydrochloride

WB

    Cabozantinib hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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

    Voir tous les produits spécifiques à Isoform VEGFR:

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

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    Axl Mer Tyro3

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    Description

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

    IC50 & Target

    VEGFR2

    0.035 ± 0. nM (IC50)

    Axl

     

    Flt-4

    6 nM (IC50)

    Flt-1

    12 nM (IC50)

    In Vitro

    Cabozantinib hydrochloride 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 hydrochloride (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 hydrochloride (0-370 nM, 24 h) inhibits cellular migration and invasion[1].
    Cabozantinib hydrochloride (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 hydrochloride 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 hydrochloride (100 mg/kg, Orally, once) inhibits MET and VEGFR2 phosphorylation in mice[1].
    Cabozantinib hydrochloride (100 mg/kg, Orally, once) significantly increases tumor hypoxia and apoptosis[1].
    Cabozantinib hydrochloride (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.
    Masse moléculaire

    537.97

    Formule

    C28H25ClFN3O5
    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.Cl
    Livraison

    Room temperature in continental US; may vary elsewhere.
    Stockage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Pureté et documentation
    Références
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    Cabozantinib hydrochloride Related Classifications

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      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:

    Cabozantinib1817759-42-4XL184BMS-907351XL 184XL-184BMS907351BMS 907351VEGFRc-Met/HGFRc-KitTAM ReceptorFLT3ApoptosisVascular endothelial growth factor receptorSCFRCD117Tyro3AxlMerCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3angiogenesisantiangiogenicapoptosisMBA-MB-231B16F10 cellsA431HT1080Inhibitorinhibitorinhibit

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