APS-2-79

• CAT Number: I013748
• CAS Number: 2002381-31-7
• Molecular Formula: C23H21N3O3.HCl
• Molecular Weight: 423.89
• Purity: ≥95%
• IUPAC Name: 6,7-dimethoxy-N-(2-methyl-4-phenoxyphenyl)quinazolin-4-amine;hydrochloride
• InChI: InChI=1S/C23H21N3O3.ClH/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);1H
• SMILES: CC1=C(C=CC(=C1)OC2=CC=CC=C2)NC3=NC=NC4=CC(=C(C=C43)OC)OC.Cl

Small molecule that stabilizes the KSR (Kinase suppressor of Ras) inactive state and antagonizes oncogenic Ras signalling (IC50 value 120 nM against ATP-biotin probe-labelling of KSR2). Furthermore, APS-2-79 modulates KSR-dependent MAPK signaling, and increases the potency of several MEK inhibitors, specifically within Ras-mutant cell lines by antagonizing release of negative feedback signaling.
KEYWORDS: APS-2-79 | supplier | KSR/Raf inhibitor | APS2-79 | CAS [2002381-31-7] | [ 2002381-25-9] | MEK | KSR2 | Kinase suppressor of Ras | Raf | MAPK | K-Ras | mitogen activated | oncogenic

Reference

NS Dhawan et al. Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Nature. 2016 Aug 24;537(7618):112-116.