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APS-2-79

Chemical Structure : APS-2-79

CAS No.: 2002381-25-9

APS-2-79 (APS 2-79;APS2-79)

Catalog No.: PC-42215Not For Human Use, Lab Use Only.

APS-2-79 is 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).

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Biological Activity

APS-2-79 is 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).
APS-2-79 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.
APS-2-79 enhances the efficacy of Trametinib against cancer cell lines containing K-Ras mutations.

Physicochemical Properties

M.Wt 387.4312
Formula C23H21N3O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 33 mg/mL

Chemical Name/SMILES

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

References

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

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