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SU11274
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SU11274图片
CAS NO:658084-23-2
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
25mg电议
100mg电议

产品介绍

化学性质

Physical AppearanceA solid
StorageStore at -20°C
M.Wt568.09
Cas No.658084-23-2
FormulaC28H30CIN5O4S
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
Canonical SMILESCC1=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。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

资料参考

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.

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.

生物活性

DescriptionSU11274是MET酪氨酸激酶的选择性抑制剂,IC50值为10 nM。
靶点MET     
IC5010 nM