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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Protein Tyrosine Kinase/PTK > SU 11274CAS：658084-23-2
Molecular Formula：C28H30CIN5O4S
Molecular Weight：568.09
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to yellow Solid
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| CAS | 658084-23-2 |
| Name | SU 11274 |
| Molecular Formula | C28H30CIN5O4S |
| Molecular Weight | 568.09 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD08276928 |
| SMILES | O=S(C1=CC2=C(C=C1)NC(/C2=C/C3=C(C(C(N4CCN(CC4)C)=O)=C(N3)C)C)=O)(N(C)C5=CC=CC(Cl)=C5)=O |
| Target Point | c-Met/HGFR |
| Passage | Protein Tyrosine Kinase/RTK |
| Background | SU11274 is a selective Met inhibitor. |
| Biological Activity | SU11274 是一种选择性的 Met 抑制剂, IC50 值为 10 nM, 对 PGDFRβ, EGFR 或 Tie2 没有抑制作用[1]。 |
| IC50 | IC50: 10nM (Met) [1] |
| In Vitro | 与其他酪氨酸激酶如FGFR-1，c-src，PDGFbR和EGFR相比，SU11274对Met与Flk的选择性大于50倍，选择性大于500倍。 SU11274抑制PI3K途径的关键调节因子的磷酸化，包括AKT，FKHR或GSK3β。 SU11274处理以剂量依赖性方式抑制TPR-MET转化的BaF3细胞的生长，在不存在白细胞介素3的情况下IC50 <3μM，而对其他致癌酪氨酸激酶(包括BCR-ABL)转化的BaF3细胞没有生长抑制作用，TEL-JAK2，TEL-ABL和TEL-PDGFβR。除细胞生长外，SU11274处理显着抑制BaF3的迁移。 TPR-MET细胞分别在1μM和5μM时分别为44.8％和80％。 SU11274抑制HGF依赖性Met的磷酸化以及HGF依赖性细胞增殖和运动，IC50为1-1.5μM。在具有功能性Met受体的H69和H345细胞中，SU11274抑制HGF诱导的细胞生长，IC50分别为3.4μM和6.5μM。 SU11274诱导G1细胞周期阻滞，G1期细胞在5μM时从42.4％增加到70.6％，并在1μM时诱导caspase依赖性细胞凋亡24％[2]。 SU11274抑制表达c-Met的非小细胞肺癌(NSCLC)细胞的细胞活力，IC50值为0.8-4.4μM，并消除肝细胞生长因子诱导的c-Met磷酸化及其下游信号传导[3]。 |
| Cell Experiment | 在存在或不存在HGF的情况下将细胞暴露于各种浓度的SU11274 24，48和72小时。使用MTT测定法或台盼蓝排除法测定活细胞数。细胞周期和细胞凋亡分别通过碘化丙啶染色和膜联蛋白V阳性染色的荧光激活细胞分选仪分析来测量。 |
| Kinase Experiment | 构建嵌合蛋白，其含有与谷胱甘肽S-转移酶(GST)融合并在SF9细胞中表达的人c-Met的细胞质结构域。使用固定在微量滴定板上的无规共聚物聚(Glu：Tyr)(4：1)作为底物，将c-Met激酶GST-融合蛋白用于基于ELISA的Met生物化学测定。在含有5μMATP和10mM MnCl 2，50mM HEPES(pH 7.5)，25mM NaCl，0.01％BSA和0.1mM原钒酸钠的缓冲液中用各种浓度的SU11274测定IC 50值。激酶反应在室温下进行5分钟。使用辣根过氧化物酶缀合的抗pTyr抗体测量底物磷酸化的程度。 |
| Data Literature Source | [1]. Wang X， et al. 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， 2 (11) :1085-1092. [2]. Sattler M， et al. A novel small molecule met inhibitor induces apoptosis in cells transformed by the oncogenic TPR-MET tyrosine kinase. Cancer Res， 2003， 63 (17) ， 5462-5469. [3]. Ma PC， et al. Functional expression and mutations of c-Met and its therapeutic inhibition with SU11274 and small interfering RNA in non-small cell lung cancer. Cancer Res， 2005， 65 (4) ， 1479-1488. |
| Unit | Bottle |
| Specification | 10mg 50mg 100mg |
SU11274 是一种选择性的 Met 抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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