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SU11652
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C22H27ClN4O2
- MW: 414.93
Description
SU11652 is a multi-target receptor tyrosine kinase inhibitor active against FLT3, PDGFRβ, VEGFR2 and FGFR1, with reported IC50 values of 1.5, 3, 27 and 170 nM, respectively. It also inhibits KIT and can affect lysosomal and sphingolipid pathways at cellular concentrations.
SU11652 is used to study growth-factor receptor signaling, angiogenesis and FLT3-driven leukemia biology. Reported cellular effects include inhibition of oncogenic FLT3 signaling, lysosomal destabilization and modulation of multidrug resistance, so pathway-specific controls are useful in complex cell systems.
Key Features
- Multi-target RTK inhibitor
- IC50: 1.5 nM for FLT3 and 3 nM for PDGFRβ
- Inhibits VEGFR2, FGFR1 and KIT
- Cell-active in kinase-driven models
Applications
- FLT3 signaling & Leukemia-cell models
- PDGFR and VEGFR pathway studies
- Angiogenesis assays
- Lysosomal and multidrug-resistance research
More Information
| Parent CAS No. | 326914-10-7 |
|---|---|
| Chemical Name | (Z)-5-((5-chloro-2-oxoindolin-3-ylidene)methyl)-N-(2-(diethylamino)ethyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide |
| SMILES | C1(Cl)C=C2/C(=C/C3=C(C)C(C(=O)NCCN(CC)CC)=C(C)N3)/C(=O)NC2=CC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C22H27ClN4O2/c1-5-27(6-2)10-9-24-22(29)20-13(3)19(25-14(20)4)12-17-16-11-15(23)7-8-18(16)26-21(17)28/h7-8,11-12,25H,5-6,9-10H2,1-4H3,(H,24,29)(H,26,28)/b17-12- |
| InChiKey | XPLJEFSRINKZLC-ATVHPVEESA-N |
| CID | 5329103 |
| Short Description | RTK inhibitor |
References
- AT Liao et al. Inhibition of constitutively active forms of mutant kit by multitargeted indolinone tyrosine kinase inhibitors. Blood. 2002 Jul 15;100(2):585-93.
- L Sun et al. 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. J Med Chem. 2003 Mar 27;46(7):1116-9.
- Y Guo et al. SU11652 Inhibits tyrosine kinase activity of FLT3 and growth of MV-4-11 cells. J Hematol Oncol. 2012 Dec 6;5:72.
- AM Ellegaard et al. Sunitinib and SU11652 inhibit acid sphingomyelinase, destabilize lysosomes, and inhibit multidrug resistance. Mol Cancer Ther. 2013 Oct;12(10):2018-30.
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