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S-8803 Sunitinib, Malate Salt, >99%

[Sunitinib Maleate] [SU-11248] [Sutent]

M.W. 532.57

C22H27FN4O2•C4H6O5

[341031-54-7]

M.I. 14:  9000

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO, up to about 40 mg/mL; very poorly soluble in water or ethanol.  Disposal:  A

View the MSDS for this product

• Sunitinib and its active metabolite (SU012662) are selective inhibitors of multiple receptor tyrosine kinases, including platelet-derived growth factor receptor and vascular endothelial growth factor receptor, that are associated with tumor growth and angiogenesis.  Deeks, E.D. and Keating, G.M.  "Sunitinib."  Drugs 66:  2255-2266 (2006).

• Sunitinib is a potent inhibitor of colony-stimulating factor-1 receptor kinase in an enzyme assay, with an IC50 value of 7 nM, and inhibits receptor phosphorylation in a cellular assay with an IC50 value of 61 nM.  Guo, J., et al.  "Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors."  Mol. Cancer Ther. 5:  1007-1013 (2006).

• Sunitinib dose-dependently inhibited stem cell factor (SCF)-induced phosphotyrosine levels on KIT (IC50 = 1 - 10 nM) and reduced SCF-stimulated ERK1/2 phosphorylation with an IC50 value consistent with that for inhibition of KIT phosphotyrosine levels. Sunitinib also inhibited SCF-stimulated proliferation in NCI-H526 cells (IC50 = 2 nM).  Abrams, T.J., et al.  "SU11248 Inhibits KIT and Platelet-derived Growth Factor Receptor β in Preclinical Models of Human Small Cell Lung Cancer."  Mol. Cancer Ther. 2:  471-478 (2003).

• Sunitinib dose-dependently inhibited FLT3-ITD phosphorylation (IC50 = 50 nM) following a 2-hour treatment. For the FLT3-ITD cell line MV-4-11, which expresses FLT3-ITD mutant, sunitinib dramatically inhibited cellular proliferation with an IC50 of 1 to 10 nM.  O'Farrell, A., et al.  "SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo."  Blood 101:  3597-3605 (2003).

• Sunitinib is the active ingredient in the drug sold under the trade name Sutent.  This drug is a small molecule receptor tyrosine kinase inhibitor that is approved for the treatment of patients having gastrointestinal stromal tumors (GIST) or renal cell carcinoma (RCC).

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

• This 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) Section 68B of the Patents Act of 1953 in New Zealand; (vi) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (vii) 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.