APS-2-79 hydrochloride( APS 2-79 hydrochloride )

Catalog No. M13126 CAS No. 2002381-31-7

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Product Name

APS-2-79 hydrochloride
Note

Research use only, not for human use.
Brief Description

A small molecule compound that modulates KSR-dependent MAPK signalling by antagonizing RAF heterodimerization.
Description

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.
In Vitro

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.
In Vivo

——
Synonyms

APS 2-79 hydrochloride
Pathway

MAPK/ERK Signaling
Target

MEK
Recptor

KSR2
Research Area

Cancer
Indication

——

CAS Number

2002381-31-7
Formula Weight

423.89208
Molecular Formula

C23H22ClN3O3
Purity

>98% (HPLC)
Solubility

DMSO
SMILES

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

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

1. Dhawan NS, et al. Nature. 2016 Sep 1;537(7618):112-116.

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