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676487  VEGFR2 Kinase Inhibitor III

3-[(2,4-Dimethylpyrrol-5-yl)methylidene]-indolin-2-one, SU5416, Vascular Endothelial Growth Factor Receptor 2 Kinase Inhibitor III, VEGFR Tyrosine Kinase Inhibitor XIV

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26 May 2012

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676487-1MG  1 mg 
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A cell-permeable indolinone compound that acts as a selective, reversible, and ATP-competitive inhibitor of VEGF-R (KDR/Flk-1) and PDGF-R tyrosine kinases (IC50 = 1.04 µM and 20 µM in NIH 3T3 cells overexpressing Flk-1; Km = 530 nM for ATP). Also potently inhibits the proliferation of HUVECs induced by VEGF, bFGF, or ECGS (IC50 = 50 nM, 5.3 µM and 30.5 µM, respectively). Blocks the autophosphorylation of internal tandem duplication (ITD) and wild type Fms-like tyrosine kinase 3 (FLT3) with an IC50 of 0.1 µM. Does not affect the EGF- or FGF- receptor tyrosine kinases activities even at 100 µM concentration. Reported to induce apoptosis and inhibit VEGF-dependent mitogenesis of human endothelial cells. A 10 mM (500 µg/210 µl) solution of VEGF Receptor 2 Kinase Inhibitor III (Cat. No. 676498) in DMSO is also available.
Product information
Form Yellow orange solid
Primary Target VEGF-R (KDR/Flk-1) and PDGF-R tyrosine kinases
Primary Target IC50 1.04 µM and 20 µM in NIH 3T3 cells overexpressing Flk-1; Km = 530 nM for ATP
Secondary target proliferation of HUVECs induced by VEGF, bFGF, or ECGS (IC50 = 50 nM, 5.3 µM and 30.5 µM, respectively
Molar mass 238.3
Protect from Light Yes
Packaged under inert gas Yes
Cell permeable Yes
ATP Competitive Yes
Purity ≥97% by HPLC
Solubility DMSO
Chemical formula C15H14N2O
CAS number 204005-46-9
Store and ship information
Storage +2°C to +8°C
Ship Ambient Temperature Only
Standard Handling
VEGFR2 Kinase Inhibitor III, molecular structure

© Merck KGaA, Darmstadt, Germany, 2012

All references to Merck refer to Merck KGaA, Darmstadt, Germany.


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