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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Cited by 19 Publications

8 Customer Reviews

  • Level of phospho-proteins in RTK and PI3K/Akt/mTOR pathways in treated tumors, detected with western blot. (c) Phospho-Erk and phospho-S6 intensity in MDSCs when co-transfected with ERK2 and p70S6K, detected with western blot.

    Nature, 2017, 543(7647):728-732. Cabozantinib (XL184, BMS-907351) purchased from Selleck.

    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.

  • Immunoblots of whole cell lysates from (A) LC2/ad NSCLC cells treated with BLU-667, cabozantinib, or vandetanib at indicated concentrations (nmol/L) for 90 minutes. Phospho- and total RET, SHC, and ERK1/2 were interrogated. In LC2/ad cells, pERK is represented by the top two bands of the triplet.

    Cancer Discov, 2018, 8(7):836-849. Cabozantinib (XL184, BMS-907351) purchased from Selleck.

    Imaging and quantification of cabozantinib (XL-184) effects on EMT in vitro. A-C, Western blot analysis of E-cadherin and c-Met expression in the XL-184-treated RFPþ tumor cells. D-F, GFP imaging merged with bright field view of the XL-184–treated RFPþ tumor cells.

    Cancer Res, 2016, 76(8):2094-104. Cabozantinib (XL184, BMS-907351) purchased from Selleck.

  • Cabozantinib specifically inhibited the phosphorylation of FLT3 (A) and downstream signaling molecules such as STAT5, Akt and ERK1/2 in FLT3-ITD MV4-11 cells (B). By contrast, the phosphorylation of downstream FLT3 signaling molecules was unaffected by cabozantinib in FLT3 wild-type OCI-AML3 cells (C). Cells were treated with cabozantinib for 2 h, and the expression of pFLT3, FLT3, pSTAT5, STAT5, pAkt, Akt, pErk1/2, and Erk1/2 was measured by Western blotting.

    Cancer Lett, 2016, 376(2):218-25. 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

Choose Selective VEGFR Inhibitors

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)
0.035 nM 1.3 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  MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUS4Z5JPOC5yMT2xNEDPxE1? NETrTZFFVVOR NHH3T|hKSzVyPUi5JI5O MlzSNlM1QDRyME[=
SNU-5  M2K5emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlf2TWM2OD1iMUmgcm0> NGOyTXEzOTl{NkG5NS=>
Hs746T  Mly0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7nd5ZKSzVyPUmuPUBvVQ>? NYfTeWZNOjF7Mk[xPVE>
SNU-1  MlzBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\scJBMUUN3ME21NlI{KG6P M3H0NFIyQTJ4MUmx
SNU-16 M37VbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTFzNEmgcm0> M2rSO|IyQTJ4MUmx
MDA-MB-231 NIDXRYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rNeWlEPTB;IE[0NlEhdk1? Mnj3NlE6OjZzOUG=
U87MG M4jXe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHi0e4tKSzVyPUG4OVEhdk1? MlnlNlE6OjZzOUG=
H441  NHfUb|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlv3TWM2OD1{MUewNEBvVQ>? M4ryXlIyQTJ4MUmx
H69 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTJyMkCwJI5O MonKNlE6OjZzOUG=
PC3 M1TJU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTFyOECwJI5O NGPHUpEzOTl{NkG5NS=>
MTC-TT MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnv1TWM2OD1yLkC0JEshOC5yMzFOwG0> MVGyNVQ4ODl7NR?=
MZ-CRC M1HKXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRiB3IN88US=> NHuy[28zOTR5MEm5OS=>
TPC-1 M{PpcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHP4d3pKSzVyPUCuNFYhMyByLkCyJO69VQ>? M2\B[lIyPDdyOUm1

... 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:

[2]
+ 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:

[1]
+ 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 Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing. 		5mg/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 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
NCT03685448 Not yet recruiting Renal Cell Carcinoma|Papillary Renal Cell Carcinoma Type 1|Papillary Renal Cell Carcinoma Type 2|Chromophobe Renal Cell Carcinoma|Sarcomatoid Renal Cell Carcinoma|Xp11.2 Translocation-Related Renal Cell Carcinoma Australian and New Zealand Urogenital and Prostate Cancer Trials Group January 30 2019 Phase 2
NCT03729245 Not yet recruiting Renal Cell Carcinoma|Metastatic Renal Cell Carcinoma Nektar Therapeutics|Bristol-Myers Squibb December 2018 Phase 3
NCT03612232 Not yet recruiting Adrenocortical Carcinoma Wuerzburg University Hospital December 2018 Phase 2
NCT03690388 Recruiting Differentiated Thyroid Cancer Exelixis October 2018 Phase 3
NCT03729297 Recruiting Salivary Gland Cancer Radboud University|Ipsen September 5 2018 Phase 2
NCT03667482 Recruiting Head and Neck Squamous Cell Cancer|Recurrent Head and Neck Squamous Cell Cancer|Metastatic Head and Neck Squamous Cell Cancer Memorial Sloan Kettering Cancer Center September 7 2018 Phase 1

Tech Support

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VEGFR Signaling Pathway Map

VEGFR Inhibitors with Unique Features

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    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) 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.

  • Axitinib

    Axitinib 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).

  • Nintedanib (BIBF 1120)

    Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3.

  • Vandetanib (ZD6474)

    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.

  • Lenvatinib (E7080)

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    Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively.

  • Pazopanib HCl (GW786034 HCl)

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

    Features:A multi-kinase inhibitor.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID