GSK 1363089

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Cat.No. 6056 - GSK 1363089 | C34H34F2N4O6 | CAS No. 849217-64-7
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)
Datasheet
Citations
Reviews
Literature

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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References

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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Citations for GSK 1363089

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