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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EMD Chemicals, Inc.
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24 May 2012
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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 |
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