Testing Data
(Foretinib (GSK1363089, XL880) is a novel MET and VEGFR2/KDR kinases inhibitor with an IC50 of 0.4 and 0.8 nM for MET and KDR, respectively. Foretinib (GSK1363089, XL880) inhibits HGF receptor family tyrosine kinases with an IC50 of 3 nM for Ron. Foretinib (GSK1363089, XL880) also inhibits KDR, Flt-1, and Flt-4 with IC50 of 0.9, 6.8 and 2.8 nM, respectively. In addition, EXEL-2880 inhibits members of the platelet-derived growth factor receptor family and the angiopoietin-1 receptor Tie-2. Foretinib (GSK1363089, XL880) exhibits modest activity against fibroblast growth factor receptor 1 and epidermal growth factor receptor and is inactive against 50 serine/threonine kinases, including cyclin-dependent kinases and protein kinase C isoforms. To delineate the cellular effect of foretinib (GSK1363089, XL880), VEGF- induced extracellular signal-regulated kinase phosphorylation was used to assess the effect of the compound on phosphorylation of KDR in human umbilical vein endothelial cells that resulted in an IC50 of 16 nM. Foretinib(GSK1363089, XL880) is the 1st orally available small molecule inhibitor of Met to enter the clinic and appears to be generally well tolerated. Anti-tumor activity has been observed and Foretinib may represent an active treatment option for patients with papillary renal-cell carcinoma. [1])
Foretinib, Inhibitor
Foretinib (GSK1363089, XL880)
Purity
>99%
Synonyms
Foretinib; Foretinib (GSK1363089; XL880); inhibitor
Purity/Purification
>99%
Solubility
DMSO >=127mg/mL - Water <1mg/mL - Ethanol >=12mg/mL
Formula
C34H34F2N4O6
CAS Number
849217-64-7
Preparation and Storage
Store at-20 degree C 2 years.
Testing Data
(Foretinib (GSK1363089, XL880) is a novel MET and VEGFR2/KDR kinases inhibitor with an IC50 of 0.4 and 0.8 nM for MET and KDR, respectively. Foretinib (GSK1363089, XL880) inhibits HGF receptor family tyrosine kinases with an IC50 of 3 nM for Ron. Foretinib (GSK1363089, XL880) also inhibits KDR, Flt-1, and Flt-4 with IC50 of 0.9, 6.8 and 2.8 nM, respectively. In addition, EXEL-2880 inhibits members of the platelet-derived growth factor receptor family and the angiopoietin-1 receptor Tie-2. Foretinib (GSK1363089, XL880) exhibits modest activity against fibroblast growth factor receptor 1 and epidermal growth factor receptor and is inactive against 50 serine/threonine kinases, including cyclin-dependent kinases and protein kinase C isoforms. To delineate the cellular effect of foretinib (GSK1363089, XL880), VEGF- induced extracellular signal-regulated kinase phosphorylation was used to assess the effect of the compound on phosphorylation of KDR in human umbilical vein endothelial cells that resulted in an IC50 of 16 nM. Foretinib(GSK1363089, XL880) is the 1st orally available small molecule inhibitor of Met to enter the clinic and appears to be generally well tolerated. Anti-tumor activity has been observed and Foretinib may represent an active treatment option for patients with papillary renal-cell carcinoma. [1])
Testing Data
(Foretinib (GSK1363089, XL880) is a novel MET and VEGFR2/KDR kinases inhibitor with an IC50 of 0.4 and 0.8 nM for MET and KDR, respectively. Foretinib (GSK1363089, XL880) inhibits HGF receptor family tyrosine kinases with an IC50 of 3 nM for Ron. Foretinib (GSK1363089, XL880) also inhibits KDR, Flt-1, and Flt-4 with IC50 of 0.9, 6.8 and 2.8 nM, respectively. In addition, EXEL-2880 inhibits members of the platelet-derived growth factor receptor family and the angiopoietin-1 receptor Tie-2. Foretinib (GSK1363089, XL880) exhibits modest activity against fibroblast growth factor receptor 1 and epidermal growth factor receptor and is inactive against 50 serine/threonine kinases, including cyclin-dependent kinases and protein kinase C isoforms. To delineate the cellular effect of foretinib (GSK1363089, XL880), VEGF- induced extracellular signal-regulated kinase phosphorylation was used to assess the effect of the compound on phosphorylation of KDR in human umbilical vein endothelial cells that resulted in an IC50 of 16 nM. Foretinib(GSK1363089, XL880) is the 1st orally available small molecule inhibitor of Met to enter the clinic and appears to be generally well tolerated. Anti-tumor activity has been observed and Foretinib may represent an active treatment option for patients with papillary renal-cell carcinoma. [1])
Related Product Information for Foretinib, inhibitor
Foretinib (GSK1363089, XL880) is a novel MET and VEGFR2/KDR kinases inhibitor with an IC50 of 0.4 and 0.8 nM for MET and KDR, respectively. Foretinib (GSK1363089, XL880) inhibits HGF receptor family tyrosine kinases with an IC50 of 3 nM for Ron. Foretinib (GSK1363089, XL880) also inhibits KDR, Flt-1, and Flt-4 with IC50 of 0.9, 6.8 and 2.8 nM, respectively. In addition, EXEL-2880 inhibits members of the platelet-derived growth factor receptor family and the angiopoietin-1 receptor Tie-2. Foretinib (GSK1363089, XL880) exhibits modest activity against fibroblast growth factor receptor 1 and epidermal growth factor receptor and is inactive against 50 serine/threonine kinases, including cyclin-dependent kinases and protein kinase C isoforms. To delineate the cellular effect of foretinib (GSK1363089, XL880), VEGF-induced extracellular signal-regulated kinase phosphorylation was used to assess the effect of the compound on phosphorylation of KDR in human umbilical vein endothelial cells that resulted in an IC50 of 16 nM. Foretinib(GSK1363089, XL880) is the 1st orally available small molecule inhibitor of Met to enter the clinic and appears to be generally well tolerated. Anti-tumor activity has been observed and Foretinib may represent an active treatment option for patients with papillary renal-cell carcinoma. [1]
Product Categories/Family for Foretinib, inhibitor
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Product Notes
The Foretinib (Catalog #AAA8506342) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "Foretinib, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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