Potent, ATP-competitive and cell permeable inhibitor of tyrosine kinases (VEGF-R2 IC50=27nM, PDGF-Rβ IC50=3nM). Also inhibits wild-type and all mutant forms of Kit in mast cells (IC50's=10 to 100nM) resulting in cell cycle arrest and apoptosis. Su11652 was also shown to induce autophagy in MCF-7 cells.
Product Details
| Alternative Name: | 5-[5-Chloro-2-oxo-1,2-dihydroindol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide |
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| Formula: | C22H27ClN4O2 |
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| MW: | 414.9 |
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| CAS: | 326914-10-7 |
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| Purity: | ≥98% (HPLC) |
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| Appearance: | Orange solid. |
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| Solubility: | Soluble in DMSO (>25 mg/ml). |
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| Shipping: | Blue Ice |
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| Long Term Storage: | -20°C |
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| Use/Stability: | Stable for at least 6 months after receipt whenstored at -20°C. |
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| Handling: | Solutions can be stored at -20°C for up to 3 months. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Identification of novel autophagy regulators by a luciferase-based assay for the kinetics of autophagic flux: T. Farkas, et al.; Autophagy
5, 1018 (2009),
Abstract;
Full Text
Discovery of 5-[5-fluoro-2-oxo-1,2-dihydroindol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase: L. Sun, et al.; J. Med. Chem.
46, 1116 (2003),
Abstract;
Inhibition of constitutively active forms of mutant kit by multitargeted indolinone tyrosine kinase inhibitors: A.T. Liao, et al.; Blood
100, 585 (2002),
Abstract;
Full Text
