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S-8803 Sunitinib, Malate Salt, >99%       Prices Reduced (May 2010)

[Sunitinib Maleate] [SU-11248] [Sutent] [PHA-290940AD] [PNU-290940AD]

M.W. 532.56

C22H27FN4O2•C4H6O5

[341031-54-7]

M.I. 14:  9000

RTECS UX9356900

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 40 mg/mL; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-50 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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• 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 has been approved in at least one country for the treatment of patients having gastrointestinal stromal tumors (GIST) or renal cell carcinoma (RCC).  NOTE:  The sunitinib sold by LC Laboratories is NOT Sutent®, and is NOT for human use.

• 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) 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.