13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
在線訂購 免費訂購熱線：021-59541103 021-60443211
標簽:EMD-1214063
聯系人:高小姐
電話:021-59541103 021-60443211
手機:13585831301
Q Q： 3004967995
Email:3004967995@qq.com
詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 5mg 10mg 50mg 100mg |
| CAS | 1100598-32-0 |
| 別名 |
|
| 化學名 | 3-[1-[[3-[5-[(1-methylpiperidin-4-yl)methoxy]pyrimidin-2-yl]phenyl]methyl]-6-oxopyridazin-3-yl]benzonitrile |
| 分子式 | C29H28N6O2 |
| 分子量 | 492.57 |
| 溶解度 | ≥ 4.93 mg/mL in DMSO, <2.52 mg/mL in EtOH, <2.56 mg/mL in H2O |
| 儲存條件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述：
EMD-1214063 is a selective inhibitor of c-Met with IC50 value of 4 nM. [1]
c-Met is a RTK (receptor tyrosine kinase) which is a single chain precursor protein. The mature form of c-Met conatains alpha and beta subunits, which are disulfide linked to each other. It is normally expressed in stem cells and progenitor cells, which allows these cells to grow invasively in an embryo or regenerate damaged tissues in an adult. The c-Met is a membrane receptor which plays an important role in embryonic development and wound healing. The only known ligand of c-Met receptor is HGF (Hepatocyte growth factor). The c-MET activation by HGF triggers transphosphorylation of the Tyr 1234 and Tyr 1235. The activation of c-Met can activate multiple signal transduction pathways including RAS pathway, PI3K pathway, STAT pathway and Notch pathway. MET pathway is essential for the development of cancer through: angiogenesis, activation of key oncogenic pathways and scatter. The abnormal MET activation means poor prognosis in cancer. [2]
EMD-1214063 inhibited the kinase activity of c-Met with IC50 value of 3 nM in assay using recombinant human c-Met kinase domain. EMD-1214063 can inhibit HGF-induced c-Met phosphorylation with an average IC50 of 6 nM in A549 cells. EMD 1214063 also significantly inhibits the activation of downstream signaling pathways of c-Met including the phosphorylation of Akt, Gab-1and Erk1/2. EMD 1214063 also can inhibit the cell viability with IC40 of less than 1 nM in MKN-45 gastric cancer cells. In cancer xenograft model, EMD-1214063 significantly inhibit the c-Met phosphorylation at 3 mg/kg and inhibit tumor cell proliferation and cyclin D1 expression at 10 mg/kg.[1]
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原創作者：上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
賬 號：2169 2341 6278
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