For research use only. Not for therapeutic Use.
APS-2-79 is a KSR-dependent MEK antagonist. APS-2-79 inhibits ATPbiotin binding to KSR2 within the KSR2-MEK1 complexe with an IC50 of 120 nM. APS-2-79 makes the stabilization of the KSR inactive state antagonizes oncogenic Ras-MAPK signaling[1].
APS-2-79 (5 μM) suppresses KSR-stimulated MEK and ERK phosphorylation in 293H cells[1].
APS-2-79 (1 μM) enhances the efficacy of the clinical MEK inhibitor trametinib within cancer cell lines containing K-Ras mutations[1]
| Catalog Number | I002537 |
| CAS Number | 2002381-25-9 |
| Synonyms | 6,7-dimethoxy-N-(2-methyl-4-phenoxyphenyl)quinazolin-4-amine |
| Molecular Formula | C23H21N3O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C23H21N3O3/c1-15-11-17(29-16-7-5-4-6-8-16)9-10-19(15)26-23-18-12-21(27-2)22(28-3)13-20(18)24-14-25-23/h4-14H,1-3H3,(H,24,25,26) |
| InChIKey | PEKZLFZZBGBOPJ-UHFFFAOYSA-N |
| SMILES | CC1=C(C=CC(=C1)OC2=CC=CC=C2)NC3=NC=NC4=CC(=C(C=C43)OC)OC |
| Reference | [1]. Dhawan NS, et al. Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Nature. 2016 Aug 24;537(7618):112-116. |
