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SU11274

SU11274

Catalog No.

A2678

C-Met抑制剂

组合的产品项目
规格	价格	库存
10mM (in 1mL DMSO)	￥ 1,536.00	现货
5mg	￥ 636.00	现货
25mg	￥ 2,727.00	现货
100mg	￥ 6,500.00	Ship with 10-15 days

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背景
文献引用
化学属性
试验操作
生物活性
质量控制

背景

SU11274是Met激酶的选择性抑制剂，IC50值为10 nM[1]。

与丝氨酸/苏氨酸激酶、细胞周期蛋白依赖性激酶2（CDK2）或包括表皮生长因子受体（EGFR）和血小板衍生生长因子受体β（PDGFRβ）在内的其它受体酪氨酸激酶相比，SU11274对Met激酶显示出高的选择性[1]。

在药物敏感或耐药MET突变体的NIH3T3 细胞和人肺癌细胞系H1993中，SU11274可以抑制Met激酶酪氨酸1234/1235的自磷酸化，但是，随后剂量依赖性增加总的MET含量。使用2 μM的 SU11274处理细胞16小时，Met的泛素化减少[2]。

参考文献：
[1] Wang X1,Le P,Liang C,Chan J,Kiewlich D,Miller T,Harris D,Sun L,Rice A,Vasile S,Blake RA,Howlett AR,Patel N,McMahon G,Lipson KE. Potent and selective inhibitors of the Met [hepatocyte growth factor/scatter factor (HGF/SF) receptor] tyrosine kinase block HGF/SF-induced tumor cell growth and invasion. Mol Cancer Ther.2003 Nov;2(11):1085-92.
[2] Leiser D1,Pochon B1,Blank-Liss W1,Francica P1,Glück AA1,Aebersold DM1,Zimmer Y1,Medová M2. Targeting of the MET receptor tyrosine kinase by small molecule inhibitors leads to MET accumulation by impairing the receptor downregulation. FEBS Lett.2014 Mar 3;588(5):653-8.

文献引用

化学属性

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	568.09
Cas No.	658084-23-2
Formula	C₂₈H₃₀CIN₅O₄S
Solubility	≥28.4 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
Chemical Name	(3Z)-N-(3-chlorophenyl)-3-[[3,5-dimethyl-4-(4-methylpiperazine-1-carbonyl)-1H-pyrrol-2-yl]methylidene]-N-methyl-2-oxo-1H-indole-5-sulfonamide
SDF	Download SDF
Canonical SMILES	CC1=C(NC(=C1C(=O)N2CCN(CC2)C)C)C=C3C4=C(C=CC(=C4)S(=O)(=O)N(C)C5=CC(=CC=C5)Cl)NC3=O
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 lung cancer cell line H1993 and NIH3T3 cells expressing drug-sensitive or drug-resistant MET mutants
Reaction Conditions	0 ~ 2 μM SU11274 for 16 h incubation
Applications	SU11274 efficiently inhibited MET autophosphorylation at kinase tyrosines 1234/1235 in five out of seven cell lines that had been tested, but, concomitantly, dose-dependently increased total MET levels. Small molecule tyrosine kinase inhibitors such as SU11274 could be potentially used to explore a variety of biological events associated with MET tyrosine kinase autophosphorylation (Tyr1234/1235 residues), including cell proliferation, survival, anchorage-independent growth and changes in cellular morphology.
Note	The technical data provided above is for reference only.
	References: 1. Leiser D, Pochon B, Blank-Liss W, et al. Targeting of the MET receptor tyrosine kinase by small molecule inhibitors leads to MET accumulation by impairing the receptor downregulation. FEBS Letters, 2014, 588(5): 653-658.