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Foretinib

Cat. No. M1758
Foretinib Structure
Synonym:

XL880, GSK1363089

Size Price Availability Quantity
10mg USD 80 In stock
50mg USD 220 In stock
100mg USD 380 In stock
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Quality Control
Biological Activity

Foretinib is an oral multikinase inhibitor targeting Met, RON, Axl, and vascular endothelial growth factor receptor. Foretinib (XL880, GSK1363089) inhibits HGF receptor family tyrosine kinases with an IC50 of 3 nM for Ron. Foretinib (XL880, GSK1363089) also inhibits KDR, Flt-1, and Flt-4 with IC50 of 0.9, 6.8 and 2.8 nM, respectively. In addition, EXEL-2880 inhibits members of the platelet-derived growth factor receptor family and the angiopoietin-1 receptor Tie-2. Foretinib (XL880, GSK1363089) is the 1st orally available small molecule inhibitor of Met to enter the clinic and appears to be generally well tolerated.

Protocol
Cell Experiment
Cell lines B16F10 cells
Preparation method HGF-induced migration assay. B16F10 cells (2 *105) were seeded onto 0.8 Am membranes in the top chamber of a 96-well Transwell plate in DMEM containing a serial dilution of EXEL-2880 and 0.1% FBS. DMEM containing HGF (50 ng/mL), 0.2% FBS, and EXEL-2880(foretinib) was added to the bottom chamber, and after 24 h, the medium was removed and Accutase (ISC BioExpress) was added to the bottom chamber. After 30 min, cells were transferred to a V-bottomed 96-well plate, centrifuged, and resuspended in HBSS containing 2 mg/mL calcein-AM (Molecular Probes). After incubation for 30 min, cells were transferred into a black 96-well plate. Fluorescence emission was measured at 480 nm using an excitation wavelength of 520 nm and imaged with a fluorescence microscope.
Concentrations 14, 41, 123nM
Incubation time 24h
Animal Experiment
Animal models ligand (e.g., HGF or VEGF)–induced receptor phosphorylation of Met in liver and Flk-1/KDR in lung
Formulation 0.9% saline
Dosages 100 mg/kg
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 632.65
Formula C34H34F2N4O6
CAS Number 849217-64-7
Purity 100.00%
Solubility DMSO
Storage at -20°C
References

Phase II trial of single-agent foretinib (GSK1363089) in patients with recurrent or metastatic squamous cell carcinoma of the head and neck.
Seiwert T et al. Invest New Drugs. 2012 Aug 24. PMID: 22918720.

Foretinib demonstrates anti-tumor activity and improves overall survival in preclinical models of hepatocellular carcinoma.
Huynh H et al. Angiogenesis. 2012 Mar;15(1):59-70. PMID: 22187171.

Foretinib (GSK1363089), a multi-kinase inhibitor of MET and VEGFRs, inhibits growth of gastric cancer cell lines by blocking inter-receptor tyrosine kinase networks.
Kataoka Y et al. Invest New Drugs. 2012 Aug;30(4):1352-60. PMID: 21655918.

Foretinib (GSK1363089), an orally available multikinase inhibitor of c-Met and VEGFR-2, blocks proliferation, induces anoikis, and impairs ovarian cancer metastasis.
Zillhardt M et al. Clin Cancer Res. 2011 Jun 15;17(12):4042-51. PMID: 21551255.

Synergistic effects of foretinib with HER-targeted agents in MET and HER1- or HER2-coactivated tumor cells.
Liu L et al. Mol Cancer Ther. 2011 Mar;10(3):518-30. PMID: 21252284.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Foretinib, XL880, GSK1363089 supplier, c-Met, inhibitors

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