SU11274
作者：齊岳
發布時間：2023-08-25
09:08:27
點擊數：
產品名稱：SU11274
產品描述：
| 產品描述 | SU11274(IC50=10 nM) is a specific Met inhibitor. It shows no significant effects on PGDFRβ, EGFR or Tie2. |
| 靶點活性 | Met:0.01 μM |
| 體內活性 | SU11274抑制PI3K通路關鍵調節器的磷酸化, 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。 |
| 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. |
| 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) |
| 別名 | Met Kinase Inhibitor, PKI-SU11274 |
| 分子量 | 568.09 |
| 分子式 | C28H30ClN5O4S |
| CAS No. | 658084-23-2 |
存儲
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: <1 mg/mL
Ethanol: 2 mg/mL (3.52 mM)
DMSO: 85 mg/mL (149.6 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
聯系我們：
郵箱：2519696869@qq.com
QQ: 2519696869
電話：18066853083
微信：18066853083
公司介紹：
西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業務范圍包括化學試劑和產品的研發、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發，涵蓋生物科技、化學品、中間體和化工材料等領域。
主營產品：COF、MOF單體系列：三蝶烯衍生物、金剛烷衍生物、四苯甲烷衍生物、peg、上轉換、石墨烯、光電材料、點擊化學、凝集素、載玻片、蛋白質交聯劑、脂質體、蛋白、多肽、氨基酸、糖化學等。
