Cabozantinib (XL184, BMS-907351)

Catalog No.S1119

Cabozantinib (XL184, BMS-907351) Chemical Structure

Molecular Weight(MW): 501.51

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.

Size Price Stock Quantity  
In DMSO USD 220 In stock
USD 110 In stock
USD 170 In stock
USD 470 In stock
USD 997 In stock

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4 Customer Reviews

  • Effects of AXL inhibitors on induction of pAKT and rescue of pERK following AXL overexpression. R428, 500 nmol/L; XL184, 3 umol/L; XL880, 100 nmol/L; in the presence or absence of 2 umol/L PLX4720. shAXL is a positive control.

    Cancer Discov 2014 4(7), 816-27. Cabozantinib (XL184, BMS-907351) purchased from Selleck.

    Cabozantinib reduces viability and spheroid and colony formation of GCTB stromal cells. (a) Adherent-growing GCTB stromal cells derived from three different patients were left untreated (CO) or were treated with cabozantinib (10 uM, XL184) or methotrexate (100 uM, MTX). Seventy-two hours later, the viability was measured by the MTT assay, and the control was set to 100%. (b) Spheroidal cultures were established as described in b. After spheroid formation, the cells were left untreated or were treated as described above. Seven days later, spheroids were photographed, and the number and volume of spheroids (spheroid surface) were determined. The data shown are the MD. (*P<0.05; **P<0.01).

    Cell Death Dis 2014 5, e1471. Cabozantinib (XL184, BMS-907351) purchased from Selleck.

  • The effect of cabozantinib on the accumulation of Dox and Rho123. (A) Fluorescence microscopy observation of the accumulation of Dox and Rho123. The scale bars represent 100 uM. (B) The accumulation of Dox and Rho123 was measured by flow cytometric analysis. The data were analysed using Kaluza software and are presented as fold-change in fluorescence intensity relative to the control HepG2/adr cells. The results are shown as the mean ± SD of three independent trials. *P < 0.05 vs. the control group.

    Liver Int 2014 10.1111/liv.12524. Cabozantinib (XL184, BMS-907351) purchased from Selleck.

    Inhibition of breast cancer cell growth using XL184. MCF-7 breast cancer cells were treated with increasing concentrations of XL-184 for 5 days. Cell number was measured  using a colorimetric growth assay (crystal violet stain) and expressed relative to DMSO treated control cells.

     

    Christina W Yde/CDM Danish Cancer Society Research Center Denmark. Cabozantinib (XL184, BMS-907351) purchased from Selleck.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description 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.
Targets
VEGFR2/KDR [1]
(Cell-free assay)
c-Met [1]
(Cell-free assay)
Kit [1]
(Cell-free assay)
VEGFR3/FLT4 [1]
(Cell-free assay)
Axl [1]
(Cell-free assay)
0.035 nM 1.3 nM 4.6 nM 6.0 nM 7.0 nM
In vitro

XL184 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] XL184 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. XL184 also induces marked inhibition of Met and VEGFR2 phosphorylation in cytokine-stimulated human umbilical vein endothelial cells (HUVECs). Although XL-184 has no significant effect on MPNST cell growth at 0.1 μM, XL184 at 5-10 μM significantly inhibits the MPNST cell growth. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
E98NT  MkjoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLte3BCOC5yMT2xNEDPxE1? NGfUO3BFVVOR NIi3SHhKSzVyPUi5JI5O NWPseolLOjN2OESwNFY>
SNU-5  NWX6OYRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRSBzOTDuUS=> Mnj6NlE6OjZzOUG=
Hs746T  NXrwb4k4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrVTWM2OD17Lkmgcm0> MUeyNVkzPjF7MR?=
SNU-1  NUnORW8{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXr0bIc1UUN3ME21NlI{KG6P MXqyNVkzPjF7MR?=
SNU-16 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVuxZmFqUUN3ME2xNVQ6KG6P Mmn3NlE6OjZzOUG=
MDA-MB-231 NE\teJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDH[VNKSzVyPTC2OFIyKG6P M{jsVFIyQTJ4MUmx
U87MG M3X2SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLxTWM2OD1zOEWxJI5O NUjrOY1ROjF7Mk[xPVE>
H441  NUPvemN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7HTWM2OD1{MUewNEBvVQ>? M3;XU|IyQTJ4MUmx
H69 NXL2enVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXp[mJnUUN3ME2yNFIxOCCwTR?= Mn;JNlE6OjZzOUG=
PC3 M2LVfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLId2RKSzVyPUGwPFAxKG6P NVPvUWlqOjF7Mk[xPVE>
MTC-TT NW\3OldKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3no[2lEPTB;MD6wOEAsKDBwMEOg{txO Mof6NlE1PzB7OUW=
MZ-CRC MkTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRiB3IN88US=> M{joU|IyPDdyOUm1
TPC-1 MkLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTBwME[gL{AxNjB{IN88US=> NX[2NVRWOjF2N{C5PVU>

... Click to View More Cell Line Experimental Data

In vivo XL184 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. XL184 also decreases invasiveness of primary tumors and reduces metastasis. [1] XL184 at 30 mg/kg/day significantly abrogates human MPNST xenografts growth and metastasis in SCID mice. [2] Administration of XL184 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 XL184 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
+ Expand
  • 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 XL184 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
+ Expand
  • Animal Models: RIP-Tag2 transgenic mice in a C57BL/6 background with spontaneous pancreatic islet tumors
  • Formulation: Suspended at a concentration of 5 mg/mL in sterile saline or water
  • Dosages: ~60 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (199.39 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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 501.51
Formula

C28H24FN3O5

CAS No. 849217-68-1
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02216578 Not yet recruiting Metastatic Gastrointestinal Stromal Tumor European Organisation for Research and Treatment of Cancer - EORTC May 2016 Phase 2
NCT02761057 Recruiting Recurrent Renal Cell Carcinoma|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer|Type 1 Papillary Renal Cell Carcinoma|Type 2 Papillary Renal Cell Carcinoma National Cancer Institute (NCI) April 2016 Phase 2
NCT02132598 Recruiting Non Small Cell Lung Cancer (NSCLC)|Metastases to the Brain Liza Villaruz, MD|Exelixis|University of Pittsburgh December 2015 Phase 2
NCT02592356 Recruiting Advanced Cancers|Endocrine Tumor M.D. Anderson Cancer Center November 2015 --
NCT02496208 Recruiting Malignant Reproductive System Neoplasm|Malignant Urinary System Neoplasm|Metastatic Urethral Neoplasm|Metastatic Urothelial Carcinoma of the Renal Pelvis and Ureter|Progressive Neoplastic Disease|Recurrent Bladder Carcinoma|Recurrent Urethra Carcinoma|Recurrent Urothelial Carcinoma of the Renal Pelvis and Ureter|Regional Urothelial Carcinoma of the Renal Pelvis and Ureter|Solid Neoplasm|Stage III Bladder Urothelial Carcinoma|Stage III Urethral Cancer|Stage IV Bladder Urothelial Carcinoma|Stage IV Urethral Cancer|Urethral Urothelial Carcinoma National Cancer Institute (NCI) July 2015 Phase 1
NCT02315430 Suspended Fallopian Tube Clear Cell Adenocarcinoma|Ovarian Clear Cell Adenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma National Cancer Institute (NCI) April 2015 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID