Sunitinib malate
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
Purity: ≥99%
Biological Activity
Sunitinib malate is a 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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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.
Mendel et al.
Clin.Cancer Res., 2003;9:327 -
SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo.
O'Farrell et al.
Blood, 2003;101:3597 -
Molecular basis for suni. efficacy and future clinical development
Faivre et al.
Nat.Rev.Drug Discov., 2007;6:734
Product Datasheets
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Citations for Sunitinib malate
The citations listed below are publications that use Tocris products. Selected citations for Sunitinib malate include:
4 Citations: Showing 1 - 4
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Feedback circuitry between miR-218 repression and RTK activation in glioblastoma.
Authors: Mathew Et al.
Cell Death Differ 2015;8:ra42
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VEGF???-conjugated mesoporous silica nanoparticle: a tumor targeted drug delivery system.
Authors: Goel Et al.
ACS Appl Mater Interfaces 2014;6:21677
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Expression of the essential Kinase PfCDPK1 from Plasmodium falciparum in Toxoplasma gondii facilitates the discovery of novel antimalarial drugs.
Authors: Gaji Et al.
Antimicrob Agents Chemother 2014;58:2598
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Gleevec/imatinib, an ABL2 kinase inhibitor, protects tumor and endothelial cells from semaphorin-induced cytoskeleton collapse and loss of cell motility.
Authors: Procaccia Et al.
Biochem Biophys Res Commun 2014;448:134
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