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SU6656

SU6656

Catalog No.

B5839

Src 酪氨酸激酶抑制剂

组合的产品项目
规格	价格	库存
10mM (in 1mL DMSO)	￥ 800.00	现货
5mg	￥ 618.00	现货
25mg	￥ 1,890.00	现货
100mg	￥ 5,072.00	现货

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背景
文献引用
化学属性
试验操作
质量控制

背景

SU6656是Src酪氨酸激酶的小分子强效选择性抑制剂.

Src(原癌基因酪氨酸蛋白激酶)是非受体蛋白酪氨酸激酶家族,包括9名成员,促进存活\血管生成\细胞增殖和侵袭途径.

在NIH 3T3细胞中,SU6656抑制PDGF-/Src驱动的有丝分裂以及PDGF刺激的c-Myc诱导[1].在UT-7/TPO中,SU6656引起细胞分裂停止,但有丝分裂引起的DNA继续积累,它也增加细胞表面CD41和CD61的表达[2].SU6656与辐射共同作用可降低内皮细胞的克隆存活.SU6656通过抑制Src家族激酶,从而减弱辐射诱导的Akt磷酸化,增加辐射诱导的细胞凋亡和血管内皮破坏[3].

在体实验,照射前给药SU6656显著促进辐射诱发的肿瘤窗口内血管破坏.照射期间给药也有助于延迟肿瘤生长[3].

参考文献：
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.

文献引用

1. Tian Y, Guo H, et al. "Nestin protects podocyte from injury in lupus nephritis by mitophagy and oxidative stress." Cell Death Dis. 2020;11(5):319. PMID:32371936

化学属性

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
运输条件	蓝冰运输或根据您的需求运输。
一般建议	不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

试验操作

Cell experiment:[1]
Cell lines	Human umbilical vein endothelial cells
Reaction Conditions	1 μM SU6656
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]
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
Dosage form	25 mg/kg in tumor volume study and 33 mg/kg in tumor vascular window model Injected intraperitoneally
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.
Note	The technical data provided above is for reference only.
	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.