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Foretinib

Chemical Structure : Foretinib

CAS No.: 849217-64-7

Foretinib (XL880;GSK1363089;GSK089;EXEL-2880)

Catalog No.: PC-42535Not For Human Use, Lab Use Only.

Foretinib (XL880, GSK1363089, GSK089, EXEL-2880) is a potent, multikinase inhibitor that inhibits c-Met and VEGFR, also KIT, Flt-3, PDGFRβ, and Tie-2.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Foretinib (XL880, GSK1363089, GSK089, EXEL-2880) is a potent, multikinase inhibitor that inhibits c-Met and VEGFR, also inhibits KIT, Flt-3, PDGFRβ, and Tie-2.
Foretinib inhibits HGFR family tyrosine kinases with IC50 of 0.4 nM for Met and 3 nM for Ron, also inhibits KDR, Flt-1, and Flt-4 with IC50 of 0.9, 6.8, and 2.8 nM, respectively.
Foretinib exhibits modest activity against FGFR1 and EGFR, no activity against 50 serine/threonine kinases, including CDKs and PKC isoforms.
Foretinib inhibits cellular HGF-induced Met phosphorylation and VEGF-induced ERK phosphorylation and prevents both HGF-induced responses of tumor cells and HGF/VEGF-induced responses of endothelial cells.
Foretinib exhibits significant inhibition of tumor burden in animal model of lung metastasis.

Physicochemical Properties

M.Wt 632.6537
Formula C34H34F2N4O6
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 38 mg/mL

Chemical Name/SMILES

1,1-Cyclopropanedicarboxamide, N-[3-fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]-N'-(4-fluorophenyl)-

References

1. Qian F, et al. Cancer Res. 2009 Oct 15;69(20):8009-16.

2. Liu L, et al. Cancer Res. 2009 Sep 1;69(17):6871-8.

3. Eder JP, et al. Clin Cancer Res. 2010 Jul 1;16(13):3507-16.

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