Cabozantinib malate (XL184)

For research use only.

Catalog No.S4001

43 publications

Cabozantinib malate (XL184) Chemical Structure

CAS No. 1140909-48-3

Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis.

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Selleck's Cabozantinib malate (XL184) has been cited by 43 publications

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Biological Activity

Description Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis.
Targets
VEGFR2/KDR [1]
(Cell-free assay)		 c-Met [1]
(Cell-free assay)		 RET [1]
(Cell-free assay)		 Kit [1]
(Cell-free assay)		 Flt-4 [1]
(Cell-free assay)
0.035 nM 1.3 nM 4 nM 4.6 nM 6 nM
In vitro

Cabozantinib has weak inhibitory activity against RON and PDGFRβ with IC50 of 124 nM and 234 nM, respectivey, and has low activity against FGFR1 with IC50 of 5.294 μM. [1] Cabozantinib at low concentration (0.1-0.5 μM) is sufficient to induce marked inhibition of constitutive and inducible Met phosphorylation and its resultant downstream signaling in MPNST cells, and inhibit HGF-induced MPNST cell migration and invasion. Cabozantinib also induces marked inhibition of Met and VEGFR2 phosphorylation in cytokine-stimulated human umbilical vein endothelial cells (HUVECs). Although Cabozantinib has no significant effect on MPNST cell growth at 0.1 μM, Cabozantinib at 5-10 μM significantly inhibits the MPNST cell growth. [2]
Assay
Methods Test Index PMID
Western blot
p-MET / MET / p-ERK5 / ERK5 / DCLK1 ; 

PubMed: 28560410     


Western blot analysis of p-MET/MET ratios, p-ERK5/ERK5 ratios and DCLK1 expression in H290 and H513 cells treated with the MET inhibitor XL184 at 1 or 3 µM.

pROS1 / pERK / pSHP2 / p-STAT3 / p-AKT ; 

PubMed: 26673800     


Immunoblot analysis of ROS1, ERK1/2, SHP2, STAT3 and AKT phosphorylation from Ba/F3 CD74-ROS1 and CD74-ROS1D2033N cells after treatment with the indicated concentrations of crizotinib and cabozantinib. GAPDH expression is included as a loading control.

28560410 26673800
Growth inhibition assay
Cell viability; 

PubMed: 28560410     


Cell viability assay of six mesothelioma cell lines (H290, H513, H28, 211H, MS-1 and H2052) and one normal mesothelial cell line LP9 after treatment with the MET inhibitor XL184. 

28560410
In vivo Cabozantinib treatment at 30 mg/kg in RIP-Tag2 mice with spontaneous pancreatic islet tumors disrupts 83% of the tumor vasculature, reduces pericytes and empty basement membrane sleeves, causes widespread intratumoral hypoxia and extensive tumor cell apoptosis, and slows regrowth of the tumor vasculature after drug withdrawal, more significantly compared with XL999 that blocks VEGFR but not c-Met, leading to only 43% reduction in vascularity, suggesting that concurrent inhibition of VEGFR and other functionally relevant receptor tyrosine kinases (RTK) amplifies angiogenesis inhibition. Cabozantinib also decreases invasiveness of primary tumors and reduces metastasis. [1] Cabozantinib at 30 mg/kg/day significantly abrogates human MPNST xenografts growth and metastasis in SCID mice. [2] Administration of Cabozantinib induces dose-dependent inhibition of tumor growth in breast, lung, and glioma tumor models, in association with decreased tumor and endothelial cell proliferation as well as increased apoptosis. A single oral dose of Cabozantinib is sufficient to induce sustained tumor growth inhibition in MDA-MB-231 tumor-bearing mice and C6 tumor-bearing rats at 100 mg/kg and 10 mg/kg, respectively. [3]

Protocol

Cell Research:

[2]

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  • Cell lines: ST88-14, STS26T, and MPNST724
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 48 hours
  • Method:

    Cells are exposed to various concentrations of Cabozantinib for 48 hours. Cell growth is determined by MTS assays using CellTiter96 Aqueous Non-Radioactive Cell Proliferation Assay kit. Absorbance is measured at a wavelength of 490 nm, and the absorbance values of treated cells are presented as a percentage of the absorbance of untreated cells.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: RIP-Tag2 transgenic mice in a C57BL/6 background with spontaneous pancreatic islet tumors
  • Dosages: ~60 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (157.33 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing. 		15 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 635.59
Formula

C28H24FN3O5.C4H6O5
CAS No. 1140909-48-3
Storage powder
in solvent
Synonyms N/A
Smiles COC1=CC2=C(C=CN=C2C=C1OC)OC3=CC=C(C=C3)NC(=O)C4(CC4)C(=O)NC5=CC=C(C=C5)F.C(C(C(=O)O)O)C(=O)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04524208 Not yet recruiting Drug: Cabozantinib Neuroendocrine Tumors|Neuroendocrine Carcinoma Karsten Gavenis|University Medical Center Goettingen December 1 2020 Phase 2
NCT04300140 Not yet recruiting Drug: AVB-S6-500|Drug: Cabozantinib (Cabo) Clear Cell Renal Cell Carcinoma Aravive Inc. October 2020 Phase 1|Phase 2
NCT04454762 Not yet recruiting Drug: Cabozantinib Hepatocellular Carcinoma Johannes Gutenberg University Mainz|Interdisciplinary Center Clinical Trials (IZKS) University Medical Center Mainz August 1 2020 Phase 2
NCT04471428 Recruiting Drug: Cabozantinib|Drug: Atezolizumab|Drug: Docetaxel Carcinoma Non-Small-Cell Lung Hoffmann-La Roche|Exelixis August 29 2020 Phase 3
NCT04338269 Recruiting Drug: Atezolizumab|Drug: Cabozantinib Carcinoma Renal Cell Hoffmann-La Roche|Exelixis|Chugai August 21 2020 Phase 3

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VEGFR Signaling Pathway Map

VEGFR Inhibitors with Unique Features

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  • Most Potent VEGFR Inhibitor

    Axitinib : VEGFR1, VEGFR2, VEGFR3, IC50=0.1 nM, 0.2 nM, 0.1-0.3 nM.

  • FDA-approved VEGFR Inhibitor

    Axitinib : Approved by FDA for Renal Cell Carcinoma.

  • Classic VEGFR Inhibitor

    Dovitinib (TKI-258, CHIR-258) : Multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM.

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  • Regorafenib (BAY 73-4506)

    Regorafenib (BAY 73-4506, Fluoro-Sorafenib) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces autophagy.

  • Axitinib

    Axitinib (AG 013736) is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.

    Features:Superior as second-line therapy relative to sorafenib (current standard-of-care).

  • Cabozantinib (BMS-907351)

    Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib induces PUMA-dependent apoptosis in colon cancer cells via AKT/GSK-3β/NF-κB signaling pathway.

  • Nintedanib (BIBF 1120)

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    Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).

  • Lenvatinib (E7080)

    Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Lenvatinib (E7080) also inhibits FGFR1-4, PDGFR, KIT, RET, and shows potent antitumor activities. Phase 3.

  • Pazopanib

    Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID