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F-4185 Foretinib, Free Base, >99%       Prices Reduced (March 2013)      NEW!

Synonyms:  [Exel-2880] [GSK-1363089] [GSK089] [XL-880] [Exel 2880] [Exel2880] [NSC-105823] [GSK 1363089] [GSK1363089] [GSK-089] [GSK 089] [XL 880] [XL880]

M.W. 632.65

C34H34F2N4O6

[849217-64-7]

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 150 mg/mL; soluble in ethanol at 5 mg/mL with warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 5-10 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

Find and View a Certificate of Analysis for this product

View the MSDS for this product

• Foretinib, also known as EXEL-2880, XL880, and GSK1363089, is a small-molecule inhibitor of the hepatocyte growth factor (HGF) and vascular endothelial growth factor (VEGF) receptor tyrosine kinase families.

• Foretinib inhibited receptor tyrosine kinases (RTKs) in vitro with IC50 values of 0.4 nM for Met and 3 nM for Ron.  It inhibited cellular Met with IC50 values of 23 nM in PC-3 prostate cells and 21 nM in murine B16F10 melanoma cells.  It also reduced tumor cell migration, invasion, and endothelial tubule formation.  Foretinib had cytotoxic activities against a broad panel of cell lines.  It also blocked lung metastasis after the implantation of B16F10 solid tumors in mice.  Qian, F., et al.  "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:  8009-8016 (2009).

• MET-amplified tumor lines with HER1 or HER2 amplification are more sensitive to the combination of foretinib with lapatinib or erlotinib.  MET-overexpressing tumor cell lines with HER1 or HER2 amplification are less sensitive to lapatinib or erlotinib in the presence of HGF.  Foretinib can reverse the effect of HGF on lapatinib or erlotinib sensitivity in these cells.  Liu, L., et al.  "Synergistic effects of foretinib with HER-targeted agents in MET and HER1- or HER2-coactivated tumor cells."  Mol. Cancer Ther. 10:  518-530 (2011).

• Foretinib inhibits tumorigenesis and blocks invasive tumor growth in different models of ovarian cancer by affecting several critical tumor functions including inducing anoikis (anchorage-dependent programmed cell death) and inhibiting (1) c-Met activation and downstream signaling, (2) ovarian cancer cell adhesion, (3) migration and invasion, and (4) proliferation.  Zillhardt, M., et al.  "Foretinib (GSK1363089), an orally available multikinase inhibitor of c-Met and VEGFR-2, blocks proliferation, induces anoikis, and impairs ovarian cancer metastasis."  Clin. Cancer Res. 17:  4042-4051 (2011)

• Foretinib potently block multiple RTKs, including VEGF receptor and the receptor of HGF c-Met.  Inhibition of c-Met and functionally related kinases intensifies the effects of VEGF receptor blockade, which leads to regression of tumor vasculature.  You, W.K., et al.  "VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer."  Cancer Res. 71:  4758-4768 (2011).

• Foretinib caused mitotic catastrophe in chronic myelogenous leukemia cells and other cell lines by JNK-dependent inhibition of Plk1 expression and induced apoptosis via a caspase 2-mediated mechanism.  Dufies, M., et al.  "Mechanism of action of the multikinase inhibitor Foretinib."  Cell Cycle 10:  4138-4148 (2011).

• Foretinib had cytotoxic effects against gastric cancer cells harboring MET and FGFR2 amplification.  It exerted its cytotoxic effects by blocking inter-RTK signaling networks with MET or FGFR2 at their center.  Kataoka, Y., et al.  "Foretinib (GSK1363089), a multi-kinase inhibitor of MET and VEGFRs, inhibits growth of gastric cancer cell lines by blocking inter-receptor tyrosine kinase networks."  Invest. New Drugs 30:  1352-1360 (2012).

• Foretinib was shown to have significant antitumor activities in patient-derived hepatocellular carcinoma xenograft models.  Huynh, H., et al.  "Foretinib demonstrates anti-tumor activity and improves overall survival in preclinical models of hepatocellular carcinoma."  Angiogenesis 15:  59-70 (2012).

• Another CAS number previously assigned to foretinib free base , namely 937176-80-2, has been deleted by CAS and is no longer in use.

• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.

• his product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

• Not available in some countries; not available to some institutions; not available for some uses.

** Our prices are lower than other vendors', but there is no compromise in quality.  Read how we are able to accomplish this:  Product Quality Discussion.

NOTES:
1.  The purpose of our competitor price comparison tables is to enable our visitors to compare the prices and purities of products of nominally equivalent quality, for vendors whose price and purity claims are openly available from a website or catalog (without a need for the customer to contact the vendor and request a quotation in order to obtain a price and purity for a standard product size).  However, the quality comparisons in these tables are not absolute:  although our product purities are uniformly very high and are established by careful testing of every lot in our laboratories, we cannot and do not vouch for the purities claimed by other vendors in these competitor price comparison tables.  (We do carry out occasional testing of other vendors' products -- see below --  and we have found many instances where vendors' product purities are far below their claimed levels.)  Effective April 1, 2011, our price comparison tables only include products where a purity commitment is found together with sizes and prices on at least one page of the vendor's web site.

2.  Researching and compiling sizes and prices for the >160 competitive vendors and more than 175 products is an expensive and tedious task for our small company.  Thus, we typically only perform revisions of these tables annually or less frequently.  The date and source of each competitive vendor's prices is indicated at the bottom of this page.  Obviously, we make no guarantee that competitive vendor prices will remain unchanged in the interval between our annual revisions.  We may occasionally update individual competitive vendor information and add new competitive vendors as we locate them.

3.  In some circumstances we permanently remove vendors from our price comparison tables.  Circumstances that lead to permanent removal are: 

A.  If a vendor does not honor its advertised price (ignoring small price increases) for one or more products when an order is attempted.  Example:  a vendor listed a compound at $808 for 10 grams on its website price list, but quoted $4,500 per 10 grams upon our inquiry.  That vendor has been permanently removed from our price comparison tables.

B.  If, on a product-by-product basis, our analyses of a vendor's product show purities more than a few percent below the vendor's advertised purities.  Example:  a vendor advertises a purity for 97% for a compound, but repeated elemental analyses show a minimum of 9% inorganic material present, beyond any salt counterion.  Another example: an HPLC analysis at a relevant UV detector wavelength shows 92% purity for a vendor's product for which 98% purity is claimed.  We realize of course that UV absorbances for impurities can be higher than for the main compound, but our products meet our purity commitment of typically >99% irrespective of absorbance factors for impurities, and we apply that standard to products from other vendors.

C.  Again on a product-by-product basis, if a vendor makes no purity claim for a given product, then their product is not shown on that product table.

D.  If we find that, as a pattern, several of a competitive vendor's products fail to meet their advertised purity commitments by significant margins or if a vendor does not provide standard and consistent purity claims for several of its products, then that vendor is permanently removed from all of our competitor price tables.

E.  Finally, if we determine that a vendor has provided fraudulent information on its website, in its literature or on a certificate of analysis, that vendor is permanently removed from all of our price comparison tables.

4.  IMPORTANT:  The presence of a competitive vendor entry in our price comparison tables does not necessarily mean that we have analyzed any of that vendor's products for purity; indeed, in most cases we have not.

5.  Please note:  where necessary, competitor prices are rounded to the nearest whole dollar.

To the best of our knowledge, the prices listed above for our competitors' products were correct as of the dates listed below for the sources of our annual price information update process.

Pricing Sources and Dates:  LC Labs - Current, PharmBlock - website - Apr 2013, ChemieTek - website - Mar 2013, Axon Medchem - website - Mar 2013, Oakwood Products - website - Jan 2013, biorbyt.com - website - Jan 2013, Taizhou Crene Biotechnology - website - Jan 2013, Acesobio - website - Jan 2013, AbMole BioScience - website - Dec 2012, MedKoo BioSciences - website - Apr 2013, Ark Pharm - website - Dec 2012, Medchem Express - website - Jan 2013, AdooQ BioScience - website - Jan 2013, EMMX BioChemicals - website - Jan 2013, ChemScene - website - Jan 2013, Kinasechem - website - Apr 2013.