SU6656
SU6656 is a small-molecule, potent and selective inhibitor of Src tyrosine kinases.
Src (proto-oncogene tyrosine-protein kinase) is a non-receptor protein tyrosine kinase family including 9 members and promotes survival, angiogenesis, and proliferation and invasion pathways.
In NIH 3T3 cell, SU6656 inhibits PDGF-/Src-driven mitogenesis and PDGF-stimulated c-Myc induction. [1] In UT-7/TPO, SU6656 cause ceased cell division but DNA continues accumulating by endomitosis. It also increased CD41 and CD61 expression on the cell surface in. [2] SU6656 in combination with radiation decrease clonogenic survival of endothelial cells. Src family kinase inhibition by SU6656 attenuated radiation-induced Akt phosphorylation and increased radiation-induced apoptosis and vascular endothelium destruction. [3]
In vivo, SU6656 administered prior to irradiation significantly promotes radiation-induced destruction of blood vessels within the tumor windows. It also facilitates tumor growth delay when administered during fractionated irradiation. [3]
References:
1. Blake RA, Broome MA, Liu X et al. SU6656, a selective src family kinase inhibitor, used to probe growth factor signaling. Mol Cell Biol. 2000 Dec;20(23):9018-27.
2. Lannutti BJ, Blake N, Gandhi MJ et al. Induction of polyploidization in leukemic cell lines and primary bone marrow by Src kinase inhibitor SU6656. Blood. 2005 May 15;105(10):3875-8.
3. Cuneo KC, Geng L, Tan J et al. SRC family kinase inhibitor SU6656 enhances antiangiogenic effect of irradiation. Int J Radiat Oncol Biol Phys. 2006 Mar 15;64(4):1197-203.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 371.45 |
| Cas No. | 330161-87-0 |
| Formula | C19H21N3O3S |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥18.55 mg/mL in DMSO |
| Chemical Name | (Z)-2-hydroxy-N,N-dimethyl-3-((4,5,6,7-tetrahydro-1H-indol-2-yl)methylene)-3H-indole-5-sulfonamide |
| SDF | Download SDF |
| Canonical SMILES | CN(S(C1=CC(/C(C(O)=N2)=C([H])/C(N3)=CC4=C3CCCC4)=C2C=C1)(=O)=O)C |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
Human umbilical vein endothelial cells |
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Reaction Conditions |
1 μM SU6656 |
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Applications |
Clonogenic survival of endothelial cells was decreased after the combined therapy of SU6656 and radiation compared with radiotherapy alone. Furthermore, Src family kinase (SFK) inhibition by SU6656 attenuated radiation-induced Akt phosphorylation and increased radiation-induced apoptosis and vascular endothelium destruction. |
| Animal experiment:[1] | |
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Animal models |
6-week-old C57BL6 mice, with Lewis lung carcinoma cells implanted into the dorsal skin fold of mice in the window model and in the hind limb in the tumor volume model |
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Dosage form |
25 mg/kg in tumor volume study and 33 mg/kg in tumor vascular window model Injected intraperitoneally |
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Applications |
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. This study demonstrated the potential use of SFK inhibition to enhance the effects of ionizing radiation during radiotherapy. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Cuneo KC, Geng L, Tan J, et al. SRC family kinase inhibitor SU6656 enhances antiangiogenic effect of irradiation. International Journal of Radiation Oncology, Biology, Physics, 2006, 64(4): 1197-1203. |
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