Foretinib (GSK1363089, XL880), Inhibitor

Foretinib (GSK1363089, XL880)

Cat. Num. AAA384812

• Purity: >98%
• Synonyms: Foretinib (GSK1363089; XL880); GSK089; EXEL-2880; inhibitor

• Purity/Purification: >98%

• Concentration: Concentration / Solvent Volume / Mass; ; 0.1 mM - 1mg: 15.81 mL; 5mg: 79.03 mL; 10mg: 158.05 mL; ; 0.5 mM - 1mg: 3.16 mL; 5mg: 15.81 mL; 10mg: 31.61 mL; ; 1 mM - 1 mg: 1.58 mL; 5mg: 7.9 mL; 10mg: 15.81 mL; ; 5mM - 1mg: 0.32 mL; 5mg: 1.58 mL; 10mg: 3.16 mL
• Concentration Note: The above data is based on the product molecular weight 632.7. 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.
• Formula: C34H34F2N4O6
• SMILES: COC1=CC2=C(C=CN=C2C=C1OCCCN3CCOCC3)OC4=C(C=C(C=C4)NC(=O)C5(CC5)C(=O)NC6=CC=C(C=C6)F)F
• Biological Activity: Foretinib (GSK1363089), a multikinase inhibitor of c-Met and VEGFR-2, blocks proliferation, induces Anoikis, and impairs ovarian cancer metastasis.
• Targets: Target- Value; Met- IC50: 0.4nM; KDR- IC50: 0.86nM; Tie-2- IC50: 1.1nM; VEGFR3/FLT4- IC50: 2.8nM; RON- IC50: 3nM; FLT3- IC50: 3.6nM; PDGFRα- IC50: 3.6nM; Kit- IC50: 6.7nM; VEGFR1/FLT1- IC50: 6.8nM; PDGFRβ- IC50: 9.6nM; FGFR1- IC50: 660nM; EGFR- IC50: 2.99uM
• Solubility: In vitro (25°C); DMSO: 87 mg/mL (137.51 mM); Water: Insoluble; Ethanol: Insoluble ; In vivo; 30% propylene glycol, 5% Tween 80, 65% D5W: 28 mg/mL; * <1 mg/ml means slightly soluble or insoluble.; * Please note that we tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
• Preparation and Storage: Store powder at -20°C 3 years; Store solution at -20°C 6 months

Chemical Structure

Related Product Information for Foretinib (GSK1363089, XL880), inhibitor

Foretinib (GSK1363089), a multikinase inhibitor of c-Met and VEGFR-2, blocks proliferation, induces Anoikis, and impairs ovarian cancer metastasis.

References

Hayato Ogura, .et al. TKI-addicted ROS1-rearranged cells are destined to survival or death by the intensity of ROS1 kinase activity, Sci Rep, 2017, 7: 5519 PMID: 28717217
Fuse MJ, .et al. Mechanisms of Resistance to NTRK Inhibitors and Therapeutic Strategies in NTRK1-Rearranged Cancers, Mol Cancer Ther, 2017, Oct;16(10):2130-2143 PMID: 28751539
Ryohei Katayama, .et al. Cabozantinib overcomes crizotinib resistance in ROS1 fusion positive cancer, Clin Cancer Res. , 2015, Jan 1; 21(1): 166-174. PMID: 25351743