APS-2-79 hydrochloride

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

一种小分子化合物，通过拮抗 RAF 异二聚化来调节 KSR 依赖性 MAPK 信号传导。

A small molecule compound that modulates KSR-dependent MAPK signalling by antagonizing RAF heterodimerization, and the conformational changes required for phosphorylation and activation of KSR-bound MEK (KSR2 IC50=120 nM); binds to the KSR2-MEK1 complex and impedes the assembly of RAF–KSR–MEK complexes, suppresses KSR-stimulated MEK and ERK phosphorylation and suppresses oncogenic Ras mutations; enhances the efficacy of Trametinib against cancer cell lines containing K-Ras mutations.

APS-2-79 (5 μM) suppresses KSR-stimulated MEK and ERK phosphorylation in 293H cells.APS-2-79 (1 μM) enhances the efficacy of the clinical MEK inhibitor trametinib within cancer cell lines containing K-Ras mutations.

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APS 2-79 hydrochloride

MAPK/ERK Signaling

MEK

KSR2

Cancer

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2002381-31-7

423.89208

C23H22ClN3O3

>98% (HPLC)

DMSO

CC1=CC(OC2=CC=CC=C2)=CC=C1NC3=C4C=C(OC)C(OC)=CC4=NC=N3.[H]Cl

4-Quinazolinamine, 6,7-dimethoxy-N-(2-methyl-4-phenoxyphenyl)-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years