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Foretinib (GSK1363089, XL880)

Catalog No. S1111 1 Customer Review(s)

Product Citations

3 Product Citation(s)

Foretinib (GSK1363089, XL880) Chemical Structure

Bio Information

Foretinib (GSK1363089, XL880) is a novel MET and VEGFR2/KDR kinases inhibitor with an IC50 of 0.4 and 0.8 nM for MET and KDR, respectively. Foretinib (GSK1363089, XL880) inhibits HGF receptor family tyrosine kinases with an IC50 of 3 nM for Ron. Foretinib (GSK1363089, XL880) 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 (GSK1363089, XL880) exhibits modest activity against fibroblast growth factor receptor 1 and epidermal growth factor receptor and is inactive against 50 serine/threonine kinases, including cyclin-dependent kinases and protein kinase C isoforms. To delineate the cellular effect of foretinib (GSK1363089, XL880), VEGF- induced extracellular signal-regulated kinase phosphorylation was used to assess the effect of the compound on phosphorylation of KDR in human umbilical vein endothelial cells that resulted in an IC50 of 16 nM. Foretinib(GSK1363089, XL880) is the 1st orally available small molecule inhibitor of Met to enter the clinic and appears to be generally well tolerated. Anti-tumor activity has been observed and Foretinib may represent an active treatment option for patients with papillary renal-cell carcinoma. ^[1]

References:

[1] Cancer Res 2009;69:8009-8016

Chemical Information

Molecular Weight (WM):	632.65
Formula:	C₃₄H₃₄F₂N₄O₆

Solubility(R.T.:25°C):	DMSO 127mg/mL
	Water <1mg/mL
	Ethanol <1mg/mL

Quality Control

View current batch:

Purity= 97.40% H-NMR HPLC Purity= 95.04% H-NMR HPLC Purity= 99.04% H-NMR HPLC Purity= 99.06% H-NMR HPLC Purity= 99.10% H-NMR HPLC

Research Area

Protein Tyrosine Kinase >> c-Met >> c-Met Inhibitors

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Related Antibodies

Product Name	Information

Reactivity: 薛亚红

Foretinib (GSK1363089, XL880) has been referenced in 3 publications.

Activation of the AXL kinase causes resistance to EGFR-targeted therapy in lung cancer.[Zhang Z, et al. Nat Genet 2012;44(8):852-60]

PubMed: 22751098

A drug resistance screen using a selective MET inhibitor reveals a spectrum of mutations that partially overlap with activating mutations found in cancer patients.[Tiedt R, et al. Cancer Res 2011;71(15), 5255-5264]

PubMed: 21697284

Study of molecular mechanisms of sensitivity and resistance to egfr-targeted therapy in lung cancer.[Zhang Z. Submitted in partial fulfillment of the requirements for the degree of Doctor of Philosophy 2010;]

PubMed:

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;Dr. Zhang of Tianjin Medical University
Foretinib (GSK1363089, XL880) purchased from Selleck

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