Cabozantinib (XL184, BMS-907351)

Catalog No.S1119
5 5 8 Product Citations

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, respectively.

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In DMSO USD 220 In stock
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Cabozantinib (XL184, BMS-907351) Chemical Structure

Cabozantinib (XL184, BMS-907351) Chemical Structure
Molecular Weight: 501.51

Validation & Quality Control

Customer Reviews(1)

Quality Control & MSDS

Related Compound Libraries

Cabozantinib (XL184, BMS-907351) is available in the following compound libraries:

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Product Information

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  • Research Area
  • Inhibition Profile

Product Description

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, respectively.
Targets VEGFR2/KDR [1] c-Met [1] Kit [1] VEGFR3/FLT4 [1] Axl [1]

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IC50 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]
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]
Features

Protocol(Only for Reference)

Cell Assay:

[2]

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.

Animal Study:

[1]

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
Solubility 30% propylene glycol, 5% Tween 80, 65% D5W, 30 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] You WK, et al. Cancer Res, 2011, 71(14), 4758-4768.

[2] Torres KE, et al. Clin Cancer Res, 2011, 17(12), 3943-3955.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-10-24)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02216578 Not yet recruiting Metastatic Gastrointestinal Stromal Tumor European Organisation for Research and Treatment of Cance  ...more European Organisation for Research and Treatment of Cancer - EORTC January 2015 Phase 2
NCT02243605 Not yet recruiting Metastatic Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor|Metastatic Osteosarcoma|Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectod  ...more Metastatic Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor|Metastatic Osteosarcoma|Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor|Recurrent Osteosarcoma National Cancer Institute (NCI) November 2014 Phase 2
NCT02260531 Not yet recruiting Breast Cancer|Brain Tumor - Metastatic Dana-Farber Cancer Institute|Exelixis|Genentech, Inc. October 2014 Phase 2
NCT02132598 Not yet recruiting Non Small Cell Lung Cancer (NSCLC)|Metastases to the Brain Liza Villaruz, MD|Exelixis, Inc|University of Pittsburgh July 2014 Phase 2
NCT01896479 Not yet recruiting Medullary Thyroid Cancer Exelixis July 2014 Phase 4

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Chemical Information

Download Cabozantinib (XL184, BMS-907351) SDF
Molecular Weight (MW) 501.51
Formula

C28H24FN3O5

CAS No. 849217-68-1
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 100 mg/mL (199 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W 30 mg/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 Name N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

Research Area

Customer Reviews (1)


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Rating
Source Christina W Yde/CDM Danish Cancer Society Research Center Denmark. Cabozantinib (XL184, BMS-907351) purchased from Selleck
Method Cell growth assay
Cell Lines MCF-7 breast cancer cells
Concentrations 0-1.5 μM
Incubation Time 5 d
Results XL-184 potently inhibited the survival of MCF-7 cells in a dose-dependent manner.

Product Citations (8)

Tech Support & FAQs

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