| CAS NO: | 658084-23-2 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 询价 |
| 5mg | 询价 |
| 25mg | 询价 |
| 100mg | 询价 |
| 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 |
| 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 | 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。 |
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.
| 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. | |
| Description | SU11274是MET酪氨酸激酶的选择性抑制剂，IC50值为10 nM。 | |||||
| 靶点 | MET | |||||
| IC50 | 10 nM | |||||
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