| 名稱 | SU11274 |
| 描述 | SU11274 (Met Kinase Inhibitor)(IC50=10 nM) is a specific Met inhibitor. It shows no significant effects on PGDFRβ, EGFR or Tie2. |
| 細胞實驗 | Cells are exposed to various concentrations of SU11274 in the presence or absence of HGF for 24, 48, and 72 hours. The number of viable cells is determined using the MTT assay or trypan blue exclusion. Cell Cycle and apoptosis are measured by fluorescence-activated cell sorter analysis via propidium iodide staining and Annexin V-positive staining, respectively. (Only for Reference) |
| 激酶實驗 | In vitro Met kinase assay: A chimeric protein is constructed containing the cytoplasmic domain of human c-Met fused to Glutathione S-transferase (GST) and expressed in SF9 cells. The c-Met kinase GST-fusion protein is used for an ELISA-based Met biochemical assay using the random copolymer poly(Glu:Tyr) (4:1) immobilized on microtiter plates as a substrate. IC50 value is determined with various concentrations of SU11274 in a buffer containing 5 μM ATP and 10 mM MnCl2, 50 mM HEPES (pH 7.5), 25 mM NaCl, 0.01% BSA, and 0.1 mM Na orthovanadate. The kinase reaction is performed for 5 minutes at room temperature. The extent of substrate phosphorylation is measured using horseradish peroxidase-conjugated anti-pTyr antibodies. |
| 體內(nèi)活性 | SU11274抑制PI3K通路關鍵調(diào)節(jié)器的磷酸化, 包括AKT, FKHR,或GSK3β。SU11274抑制HGF依賴的Met磷酸化,及HGF依賴的細胞增殖和活動,IC50為1-1.5 μM。在TPR-MET轉化的BaF3細胞中,白細胞介素- 3存在時,用SU11274處理細胞,以劑量依賴的方式抑制細胞生長。SU11274（IC50<3 μM）則不會抑制其他致癌酪氨酸激酶轉化的BaF3細胞生長,包括BCR-ABL, TEL-JAK2, TEL-ABL,和TEL-PDGFβR。在BaF3.TPR-MET細胞中,經(jīng)SU11274處理,也顯著抑制細胞遷移,按1 μM 和5 μM處理,抑制分別為44.8% 和 80%。在具有功能性Met受體的H69和H345細胞中,SU11274抑制 HGF誘導的細胞生長,IC50分別為3.4 μM 和 6.5 μM。表達c-Met的非小細胞肺癌(NSCLC)細胞中,SU1127抑制細胞活力,IC50為0.8-4.4 μM,同時去除肝臟生長因子誘導的c-Met 及其下游信號磷酸化。 |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 2 mg/mL (3.52 mM)
DMSO : 85 mg/mL (149.6 mM)
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| 關鍵字 | SU-11274 | PKI-SU-11274 | SU11274 | Inhibitor | Autophagy | inhibit | SU 11274 | c-Met/HGFR | Apoptosis | PKI-SU 11274 |
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