APS-2-79 (hydrochloride)

APS-2-79 is an inhibitor of MAPK signaling dependent on kinase suppressor of Ras (KSR). It inhibits ATPbiotin binding to KSR2 in KSR2-MEK1 complexes (IC50 = 120 nM), stabilizes KSR2 in an inactive state, and reduces interactions between B-RAF and KSR2-MEK1 complexes. APS-2-79 (5 µM) inhibits KSR-stimulated phosphorylation of MEK and ERK in HEK293H cells. It enhances the efficacy of the MEK inhibitor trametinib (Cay-16292), further reducing cell viability in HCT116 and A549 cell lines containing K-Ras mutations, but not B-RAF mutant SK-MEL-239 and A375 cell lines, when used at a concentration of 1 µM.Formal Name: 6,7-dimethoxy-N-(2-methyl-4-phenoxyphenyl)-4-quinazolinamine, monohydrochloride. CAS Number: 2002381-31-7. Molecular Formula: C23H21N3O3 . HCl. Formula Weight: 423.9. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 25 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.3 mg/ml, Ethanol: 1 mg/ml. lambdamax: 220, 252, 342 nm. SMILES: COC1=C(OC)C=C(C(NC2=C(C)C=C(OC3=CC=CC=C3)C=C2)=NC=N4)C4=C1.Cl. InChi Code: 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. InChi Key: LIXKSHWZJNNZHG-UHFFFAOYSA-N.