產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 10mg 50mg 100mg
CAS	1391712-60-9
別名
化學(xué)名	(Z)-2-((E)-(5-chloro-2-(((S)-6-(4-(2-hydroxyethyl)piperazin-1-yl)-1-methoxy-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)amino)pyrimidin-4(3H)-ylidene)amino)-N-methylbenzimidic acid
分子式	C30H38ClN7O3
分子量	580.12
溶解度	≥ 9.25mg/mL in DMSO with gentle warming
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：

IC50: 1000 nM for the proliferation in SUM190 cell lines

The focal adhesion kinase FAK1 is a cytoplasmic tyrosine kinase that localizes to focal adhesions, and controls a number of cell pathways including proliferation, viability and survival. Anaplastic lymphoma kinase 1 (ALK-1) is a member of the insulin receptor tyrosine kinase family. ALK mutations have also been implicated in the pathogenesis of non-small cell lung cancer (NSCLC) and other solid tumors. CEP-37440 is a highly selective and potent dual inhibitor of ALK and FAK1.

In vitro: 300 nM CEP-37440 was able to decrease the proliferation of the triple negative FC-IBC02 cell line and, 1000 nM CEP-37440 was able to complete inhibit the proliferation of these cells. Genes involved in functions such as cellular growth and proliferation, cell cycle, cell death and survival and cellular movement and cell-to cell signaling and interaction were differentially regulated by CEP-37440 in sensitive IBC cell lines. Among them, TGFβ1 and MMP3 were down-regulated and DKK3, CAV1 and TFPI2 were up-regulated by CEP-37440, which might be probalby caused by its dual inhibition of ALK and FAK1 [1].

In vivo: In FC-IBC02 orthotopic breast cancer xenograft models, CEP-37440 was able to reduce the growth of the primary tumor and inhibit the development of spontaneous metastases in brain [1].

Clinical trials: CEP-37440 is a dual ALK/FAK inhibitor currently under investigation in a phase I trial to determine its MTD in patients with advanced or metastatic solid tumors (NCT01922752).

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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