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 / Product Datasheet / Safety Data Sheet

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.

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.

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

Citations are publications that use Tocris products. Selected citations for Sunitinib malate include:

Mathew et al (2015) Feedback circuitry between miR-218 repression and RTK activation in glioblastoma. Cell Death Differ 8 ra42. PMID: 25943352.

Procaccia et al (2014) Gleevec/imatinib, an ABL2 kinase inhibitor, protects tumor and endothelial cells from semaphorin-induced cytoskeleton collapse and loss of cell motility. Biochem Biophys Res Commun 448 134. PMID: 24759231.

Do you know of a great paper that uses Sunitinib malate from Tocris? If so please let us know.

View Related Products by Product Action

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

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