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 ActivityPotent, 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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.
Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor.
Molecular basis for suni. efficacy and future clinical development
Faivre et al.
Nat.Rev.Drug Discov., 2007;6:734
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
Feedback circuitry between miR-218 repression and RTK activation in glioblastoma.
Authors: Mathew Et al.
Cell Death Differ 2015;8:ra42
VEGF???-conjugated mesoporous silica nanoparticle: a tumor targeted drug delivery system.
Authors: Goel Et al.
ACS Appl Mater Interfaces 2014;6:21677
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
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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