Sunitinib malate

Cat. No. 3768

Sunitinib malate C22H27FN4O2.C4H6O5 [341031-54-7]

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Alternative Name: SU 11248

Chemical Name: N-[2-(Diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidine)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide (2S)-2-hydroxybutanedioate salt

Biological Activity

Potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor (Ki values are 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT respectively). Also inhibits cellular receptor phosphorylation of FLT3, RET and CSF-1R. Exhibits antiangiogenic and antitumor activity in multiple xenograft models.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M.Wt:
532.56
Formula:
C22H27FN4O2.C4H6O5
Solubility:
Soluble to 25 mM in DMSO
Purity:
>99 %
Storage:
Store at +4°C
CAS No:
341031-54-7

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

References

Mendel et al (2003) 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. Clin.Cancer Res. 9 327. PMID: 12538485.

O'Farrell et al (2003) SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood 101 3597. PMID: 12531805.

Faivre et al (2007) Molecular basis for sunitinib efficacy and future clinical development Nat.Rev.Drug Discov. 6 734. PMID: 17690708.

Roskoski (2007) Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor. Biochem.Biophys.Res.Comm. 356 323.

If you know of a relevant citation for this product please let us know.

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Keywords: Sunitinib malate, supplier, Potent, VEGFR, PDGRb, PDGFRbeta, PDGFRβ, FGFR, inhibitors, Vascular, Endothelial, Growth, Factor, Receptors, KDR, Flt, Flk, Kit, Receptor, Tyrosine, Kinases, RTKs, Fibroblast, platelet, derived, CD117, SU11248, Pfizer, Tocris Bioscience, VEGFR Inhibitors

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