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Foretinib is an inhibitor of ROS1, MET, Ron, Axl, Tie-2, and VEGFR2 that exhibits anticancer chemotherapeutic and anti-angiogenic activities. In subjects with squamous cell carcinoma, foretinib decreases tumor size. In hepatocellular carcinoma cells, foretinib increases expression of p27 and Bim, decreases expression of cyclin B1 and p-c-Myc, and induces G2/M phase cell cycle arrest, inhibiting cell growth and migration as well as tumor growth and angiogenesis.
| Cas No. | 849217-64-7 |
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| Purity | ≥98% |
| Formula | C34H34F2N4O6 |
| Formula Wt. | 632.65 |
| Chemical Name | 1-N'-[3-fluoro-4-[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide |
| IUPAC Name | 1-N'-[3-fluoro-4-[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide |
| Synonym | GSK-1363089, GSK1363089; XL880 |
| Solubility | Relatively insoluble in water and ethanol. Soluble in DMSO to 127 mg/mL. |
| Appearance | Off white to pale yellow powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Shah MA, Wainberg ZA, Catenacci DV, et al. Phase II study evaluating 2 dosing schedules of oral foretinib (GSK1363089), cMET/VEGFR2 inhibitor, in patients with metastatic gastric cancer. PLoS One. 2013;8(3):e54014. PMID: 23516391.
Seiwert T, Sarantopoulos J, Kallender H, et al. Phase II trial of single-agent foretinib (GSK1363089) in patients with recurrent or metastatic squamous cell carcinoma of the head and neck. Invest New Drugs. 2013 Apr;31(2):417-24. PMID: 22918720.
Huynh H, Ong R, Soo KC. Foretinib demonstrates anti-tumor activity and improves overall survival in preclinical models of hepatocellular carcinoma. Angiogenesis. 2012 Mar;15(1):59-70. PMID: 22187171.