Biological Activity
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
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 63.26 | 100 | |
| ethanol | 63.26 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 632.65. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.58 mL | 7.9 mL | 15.81 mL |
| 5 mM | 0.32 mL | 1.58 mL | 3.16 mL |
| 10 mM | 0.16 mL | 0.79 mL | 1.58 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.32 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: 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, MET, Receptors, Tocris Bioscience
