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Cat. No. Name Size Price Add Cart
KI0588Xl8805 mg$272
Xl88050 mg$1392
Xl880200 mg$3952

Chemical Characteristic

Product NameXl880
SynonymsGSK1363089, EXEL-2880, foretinib
CAS No.849217-64-7
Molecular Weight 632.65
FormulaC34H34F2N4O6
Chemical NameN-[3-Fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide
SmilesC1(CC1)(C(=O)Nc1cc(c(cc1)Oc1ccnc2c1cc(c(c2)OCCCN1CCOCC1)OC)F)C(=O)Nc1ccc(cc1)F
Chemical Structure

Biological activities

XL880 is an ATP-competitive inhibitor of MET and VEGFR2/KDR. XL880 inhibits MET and VEGFR2/KDR kinases with IC50 of 0.4 and 0.8 nM, respectively.[1] XL880 inhibits gastric cancer cell lines (MKN-45 and KATO-III) with IC50 of 8 and 30 nM, respectively. XL880 compromises cell growth through MET receptor inhibition in MKN-45 but via a different mechanism in KATO-III. XL880 inhibits phosphorylation of EGFR and HER3. [2] XL880 decreases phosphorylation status of Met, RON, ERK, and AKT, decreases tumor cell proliferation, and increases apoptosis of tumor and endothelial cells. [3] XL880 has an inhibitory activity toward KIT, Flt-3, platelet-derived growth factor receptor β, and Tie-2. In vitro, XL880 inhibits HGF-induced responses of tumor cells and HGF/VEGF- induced responses of endothelial cells. [4] XL880 has anti-tumor effects in vivo against tumors without MET or FGFR2 amplification. [2] Administration of XL880 decreases tumor staining of pMet, pRON, pERK, and pAKT. [3]

Protocols

Stock solution of XL880 is prepared in DMSO and stored at −20 °C. [2]

References

[1] Ross RW, et al. A phase II study of the c-Met RTK inhibitor XL880 in patients (pts) with papillary renal-cell carcinoma (PRC). J Clin Oncol (Meeting Abstracts). 2007: 15601.
[2] Kataoka Y, et al. Foretinib (GSK1363089), a multi-kinase inhibitor of MET and VEGFRs, inhibits growth of gastric cancer cell lines by blocking inter-receptor tyrosine kinase networks. Invest New Drugs. 2012, 30(4): 1352-1360.
[3] P LoRusso, et al. Pharmacodynamics of XL880, a novel spectrum selective kinase inhibitor (SSKI) administered orally in patients with advanced solid tumors (AST). Symposium on Molecular Targets and Cancer Therapeutics. 2006. XL880 EORTC-NCI-AACRnov06.pdf
[4] Qian F, et al. Inhibition of tumor cell growth, invasion, and metastasis by EXEL-2880 (XL880, GSK1363089), a novel inhibitor of HGF and VEGF receptor tyrosine kinases. Cancer Res. 2009, 69(20): 8009-8016.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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