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.
|Source||Blood Adv (2018). Figure 2. SU6656|
|Method||In vitro culture of CD341 HPCs into megakaryocytes|
|Cell Lines||CD341 HPCs|
|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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Human B lymphocytes and non-Hodgkin's lymphoma cells become polyploid in response to the protein kinase inhibitor SU6656.
Dussault N, et al. Blood Cells Mol Dis. 2007 Jul-Aug;39(1):130-4. PMID: 17434768.
SRC family kinase inhibitor SU6656 enhances antiangiogenic effect of irradiation.
Cuneo KC, et al. Int J Radiat Oncol Biol Phys. 2006 Mar 15;64(4):1197-203. PMID: 16504759.
Induction of polyploidization in leukemic cell lines and primary bone marrow by Src kinase inhibitor SU6656.
Lannutti BJ, et al. Blood. 2005 May 15;105(10):3875-8. PMID: 15677565.
SU6656, a selective src family kinase inhibitor, used to probe growth factor signaling.
Blake RA, et al. Mol Cell Biol. 2000 Dec;20(23):9018-27. PMID: 11074000.
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