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Submit ReviewGSK 1363089
Description: Potent inhibitor of MET, VEGFR2, Ron and AXL
Alternative Names: XL 880,EXEL 2880,Foretinib
Chemical Name: N-[3-Fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide
Purity: ≥98% (HPLC)
Biological Activity for GSK 1363089
GSK 1363089 is a potent inhibitor of MET, VEGFR2, Ron and AXL (IC50 values are 0.4, 0.9, 3 and 11 nM, respectively). Also potently inhibits Tie-2, Flt-1, Flt-3, Flt-4, KIT, PDGFRα and PDGFRβ. Inhibits migration and invasion of B16F10 melanoma cells in vitro. Suppresses B16F10 tumor growth and metastasis in mice. Orally available.
Technical Data for GSK 1363089
| M. Wt | 632.65 |
| Formula | C34H34F2N4O6 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 849217-64-7 |
| PubChem ID | 42642645 |
| InChI Key | CXQHYVUVSFXTMY-UHFFFAOYSA-N |
| Smiles | COC1=CC2=C(N=CC=C2OC3=C(C=C(C=C3)NC(C4(C(NC5=CC=C(C=C5)F)=O)CC4)=O)F)C=C1OCCCN6CCOCC6 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for GSK 1363089
References for GSK 1363089
References are publications that support the biological activity of the product.
Myers et al (2016) AXL inhibitors in cancer: A medicinal chemistry perspective. J.Med.Chem. 59 3593 PMID: 26555154
Faria et al (2015) Foretinib is effective therapy for metastatic sonic hedgehog medulloblastoma. Cancer Res. 75 134 PMID: 25391241
Qian et al (2009) 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. 69 8009 PMID: 19808973
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Keywords: GSK 1363089, GSK 1363089 supplier, GSK1363089, potent, inhibitors, inhibits, HGF, VEGFR2, AXL, tyrosine, kinases, orally, available, XL880, EXEL2880, XL, 880, EXEL, 2880, Foretinib, MET, Receptors, VEGFR, FLT3, PDGFR, 6056, Tocris Bioscience
Citations for GSK 1363089
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