l General Information |
Product Name | Foretinib (GSK1363089) |
General description | Foretinib is an orally bioavailable small molecule with potential antineoplastic activity. |
Synonym | 1-N'-[3-fluoro-4-[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide; EXEL-2880; XL-880 |
Purity | ≥98.0%(HPLC) | CAS Number | 849217-64-7 |
Formula | C34H34F2N4O6 | Molecular Weight | 632.65 |
Suitability | BioReagent, suitable for cell culture, etc. |
l Physical and Chemical Information |
Appearance | solid |
Solubility(25℃) | DMSO | ≥50mg/mL |
Ethanol | Insoluble |
Water | Insoluble |
l Biological Information |
Biochem/Physiol
Actions | Foretinib is an orally bioavailable small molecule with potential antineoplastic activity. Foretinib binds to and selectively inhibits hepatocyte growth factor (HGF) receptor c-MET and vascular endothelial growth factor receptor 2 (VEGFR2), which may result in the inhibition of tumor angiogenesis, tumor cell proliferation and metastasis. The proto-oncogene c-MET has been found to be over-expressed in a variety of cancers. VEGFR2 is found on endothelial and hematopoietic cells and mediates the development of the vasculature and hematopoietic cells through VEGF signaling. Foretinib (GSK1363089) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. |
Application | Foretinib has been used in trials studying the treatment of Cancer, Breast Cancer, Carcinoma, Renal Cell, Recurrent Breast Cancer, and Neoplasms, Head and Neck, among others. Foretinib is an orally available small molecule compound designed to target multiple RTKs implicated in the development, progression and spread of cancer. It inhibits the activation of MET, RON, ERK and AKT, decreased proliferation and increased apoptosis. |
l Storage |
Storage temp. | -20℃ |
l Precautions and Disclaimer |
This product is for R&D use only, not for drug, household, or other uses. |
l References |
1. http://www.drugbank.ca 2. https://ncit.nci.nih.gov 3. https://www.ncbi.nlm.nih.gov |
