CEP37440

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CEP-37440 是一种有效且特异性的双 FAK/ALK 抑制剂，IC50 为 120 nM（75% 人血浆中的 ALK 细胞）和 2.3 nM (FAK)。

CEP-37440 is an orally available dual kinase inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) and focal adhesion kinase (FAK), with potential antineoplastic activity. Upon administration, ALK-FAK inhibitor CEP-37440 selectively binds to and inhibits ALK kinase and FAK kinase. The inhibition leads to disruption of ALK- and FAK-mediated signal transduction pathways and eventually inhibits tumor cell growth in ALK- and FAK-overexpressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development; its dysregulation and gene rearrangements are associated with a variety of tumors.

Cell Viability Assay Cell Line:FC-IBC02, KPL4, SUM190, MDA-IBC03 and SUM149 cells Concentration:0, 300, 1000, 2000 and 3000 nM Incubation Time:0, 24, 48, 72, 96, 120, 144, 168, and 192 hours Result:Reduced the proliferation of three out of five IBC cell lines at low concentration. Inhibited the proliferation almost completely at 3000 nM concentration.Western Blot Analysis Cell Line:FC-IBC02, SUM 190, and KPL4 cells Concentration:1000 nM Incubation Time:0, 48, 72, 96 and 120 hours Result:Decreased phospho-FAK1 by half in FC-IBC02, SUM190, and KPL4 cells after 48 hours.

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CEP37440 | CEP 37440 | CEP-37440

Microbiology/Virology

HCV

ALK| FAK

Cancer

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1391712-60-9

580.12

C30H38ClN7O3

>98% (HPLC)

DMSO : ≥ 41 mg/mL. 70.68 mM

CNC(=O)c1ccccc1Nc1nc(ncc1Cl)Nc1c(c2c(C[C@H](CCC2)N2CCN(CC2)CCO)cc1)OC

(S)-2-((5-chloro-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-1-methoxy-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)amino)pyrimidin-4-yl)amino)-N-methylbenzamide

(-20℃)

With Ice Pack

≥ 2 years