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SU6656 is a small-molecule, indolinone which potently and selectively inhibits Src tyrosine kinases, which are known to function in signal transduction pathways.SU6656 can induce polyploidy in cells of lymphoid origin, revealing a chemotherapeutic potential for this inhibitor to limit tumor propagation of malignant B cell lymphomas, although not without affecting normal B cells as well.Clonogenic survival of endothelial cells was decreased after the combined therapy of SU6656 and radiation compared with radiotherapy alone.Furthermore, SFK inhibition by SU6656 attenuated radiation-induced Akt phosphorylation and increased radiation-induced apoptosis and vascular endothelium destruction.In vivo, SU6656 administered before irradiation significantly enhanced radiation-induced destruction of blood vessels within the tumor windows and enhanced tumor growth delay when administered during fractionated irradiation.SU6656 might be useful as a differentiation-inducing agent for MKs and is an important tool for understanding the molecular basis of MK endomitosis. SU6656 should prove a useful additional tool for further dissecting the role of Src kinases in this and other signal transduction pathways.
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Source | Blood Adv (2018). Figure 2. SU6656 |
| Method | In vitro culture of CD341 HPCs into megakaryocytes | |
| Cell Lines | CD341 HPCs | |
| Concentrations | 2.5 μM | |
| Incubation Time | 4 days | |
| Results | Each small inhibitor, SU6656, Y27632, and AZD1152, effects distinct intracellular pathways, yet all enhance the degree of polyploidism of the resultant megakaryocytes |
| Molecular Weight | 371.45 |
| Formula | C19H21N3O3S |
| CAS Number | 330161-87-0 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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