產(chǎn)品目錄

規(guī)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 All other available size: ship with RT , or blue ice upon request

產(chǎn)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]

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請穿好實驗服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

在線咨詢

留言注意事項：

1.遵守中華人民共和國有關法律、法規(guī)，尊重網(wǎng)上道德，承擔一切因您的行為而直接或間接引起的法律責任。

2.請您真實的反映產(chǎn)品的情況,不要捏造、誣蔑、造謠。如對產(chǎn)品有任何疑問,也可以留言咨詢。

3.未經(jīng)本站同意，任何人不得利用本留言簿發(fā)布個人或團體的具有廣告性質(zhì)的信息或類似言論。

您感興趣的產(chǎn)品*
您的單位*
聯(lián)系人*
聯(lián)系電話*
詳細地址*
常用郵箱*
請輸入您對我們的意見或建議*
驗證碼*