Sunitinib . malate

CHF 40.00
In stock
AG-CR1-3707-M0011 mgCHF 40.00
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AG-CR1-3707-M500500 mgCHF 340.00
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Product Details
Synonyms SU-11248
Product Type Chemical

C22H27FN4O2 . C4H6O5

MW 398.5 . 134.1
CAS 341031-54-7
Purity Chemicals ≥98%
Appearance Solid.
Solubility Soluble in DMSO (10mg/ml) or ethanol.
Identity Determined by 1H-NMR.
Smiles O[C@@H](CC(O)=O)C([O-])=O.[H][N+](CC)(CC)CCNC(=O)C1=C(C)NC(\C=C2/C(=O)NC3=C2C=C(F)C=C3)=C1C
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
  • Potent ATP-competitive and cell permeable multi-targeted receptor tyrosine kinase (RTK) inhibitor targeting VEGFR and PDGFR-β. Inhibits FLK1 (Ki=9nM), PDGFRβ (Ki=8nM) and FLT3. It is at least 10-fold selective for FLK1 and PDGFRβ over a variety of tyrosine kinases in a panel, including EGFR, Cdk2, Met, IGFR-1, Abl and Src.
  • Inhibits the cellular receptor phosphorylation of FLT3, RET and CSF-1R.
  • Also shown to inhibit c-Kit.
  • Exhibits potent antiangiogenic and antitumor activity in multiple xenograft models.
Product References
  1. Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase: L. Sun, et al.; J. Med. Chem. 46, 1116 (2003)
  2. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship: D. B. Mendel, et al.; Clin. Cancer Res. 9, 327 (2003)
  3. SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo: A.M. O'Farrell, et al.; Blood 101, 3597 (2003)
  4. 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: J. Guo, et al.; Mol. Cancer. Ther. 5, 1007 (2006)
  5. Molecular basis for sunitinib efficacy and future clinical development: S. Faivre, et al.; Nat. Rev. Drug Discov. 6, 734 (2007)
  6. Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor: R. Roskoski; BBRC 356, 323 (2007)
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