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APS-2-79 编号 : 6111501

化学信息

产品英文名称APS-2-79
Iupac 化学名称APS-2-79 
同义词APS 2-79 
英文同义词APS 2-79 
分子式C23H21N3O3 
分子量387.43 
InChiKey
InChi
Cas2002381-25-9

技术数据

外观crystalline solid 
纯度98% 
可溶性Soluble in DMSO 
存储3 years -20ºCpowder 
运输条件Shipped under ambient temperature as non-hazardous chemical. 
质量控制

产品详情

APS-2-79 is an antagonist of MEK phosphorylation by RAF through direct binding of the KSR active site.


APS-2-79 inhibits BRAF and CRAF phosphorylation of MEK in a KSR-dependent manner. APS-2-79 does not affect BRAF(V600E)-induced MAPK activation in cells. APS-2-79 impedes KSR-stimulated MAPK signalling within cells through wild-type and MEK(AAAA) equally. APS-2-79 synergizes with trametinib specifically in Ras-mutant cells compared to the HER-family and SRC-family inhibitors lapatinib and sarcatinib. APS-2-79 increases the potency of several MEK inhibitors specifically within Ras-mutant cell lines by antagonizing release of negative feedback signalling, demonstrating the potential of targeting KSR to improve the efficacy of current MAPK inhibitors. The IC50 value of APS-2-79 against ATPbiotin probe-labelling of KSR2 is 120 nM.


 

结构

6111501 - APS-2-79 | CAS 2002381-25-9

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