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Foretinib (GSK1363089)

  • Foretinib 200x200
  • Foretinib 600x600
Price:
$169.00
Catalog #:
C4136-5
Quantity:


Product Description

Foretinib (GSK1363089) is a potent multi-kinase inhibitor of HGFR, VEGFR, KIT, Flt, PDGFR and Tie-2. In a cell-free assay, Foretinib (GSK1363089) is most potent for Met, KDR, and Tie-2, with IC50 values of 0.4 nM, 0.86 nM, and 1.1 nM, respectively. Foretinib (GSK1363089) also inhibits Ron, Flt1/3/4, KIT, and PDGFR?/?, with higher IC50 values ranging from 3 nM to 9.6 nM. [1] It binds tightly to Met and KDR with a very slow off-rate and inhibits tumor formation in an in vivo murine model of lung metastasis. [1]
A recent report showed that Foretinib (GSK1363089), by targeting cMet, significantly reduced primary medulloblastoma growth and invasion, and increased survival in disseminated mouse models of sonic hedgehog (SHH)-driven medulloblastoma. [2]
Foretinib (GSK1363089) has been examined in multiple clinical trials in wild-range of cancer patients including metastatic breast cancer, metastatic gastric cancer, papillary renal cell carcinoma (PRC), liver cancer, non-small-cell lung cancer, and squamous cell cancer of the head and neck."


Technical information:

Chemical Formula:   C34H34F2N4O6
CAS #:   849217-64-7
Molecular Weight:   632.65
Purity:   > 98%
Appearance:   White
Chemical Name:   N-(3-fluoro-4-(6-methoxy-7-(3-morpholinopropoxy)quinolin-4-yloxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Solubility:   Up to 100 mM in DMSO
Synonyms:   Foretinib, GSK1363089,GSK 1363089, EXEL-2880, XL-880

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.


Reference:

1. 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):8009-16 Pubmed ID: 19808973
2. Faria CC, et al. Foretinib is effective therapy for metastatic sonic hedgehog medulloblastoma. Cancer Res. 2015; 75(1):134-46 Pubmed ID: 25391241
3. Study of Foretinib in Combination With Lapatinib in Patients With Metastatic Breast Cancer. clinicaltrials.gov/NCT01138384

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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