DEL-22379

DEL-22379 is an inhibitor of ERK dimerization that disrupts EGF-induced co-immunoprecipitation of ERK tagged with hemagglutinin (HA) or FLAG epitopes with an IC50 value of approximately 0.5 µM without affecting ERK phosphorylation or kinase activity (IC50s = >10 µM). It inhibits cell growth in a panel of melanoma and colorectal cancer cell lines (IC50s = 150-400 nM). DEL-22379 (15 mg/kg, i.p.) inhibits ERK dimerization in liver extract and tumor tissue and inhibits tumor progression in an A375 mouse xenograft model. It also reduces tumor growth in a BRAF mutant colorectal cancer patient-derived xenograft (PDX) mouse model.Formal Name: N-[2,3-dihydro-3-[(5-methoxy-1H-indol-3-yl)methylene]-2-oxo-1H-indol-5-yl]-1-piperidinepropanamide. CAS Number: 181223-80-3. Molecular Formula: C26H28N4O3. Formula Weight: 444.5. Purity: >98% (mixture of rotamers). Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml, Ethanol: slightly soluble. lambdamax: 224, 276, 405 nm. SMILES: O=C(NC1=CC(/C(C(N2)=O)=C/C3=CNC4=C3C=C(OC)C=C4)=C2C=C1)CCN5CCCCC5. InChi Code: InChI=1S/C26H28N4O3/c1-33-19-6-8-23-20(15-19)17(16-27-23)13-22-21-14-18(5-7-24(21)29-26(22)32)28-25(31)9-12-30-10-3-2-4-11-30/h5-8,13-16,27H,2-4,9-12H2,1H3,(H,28,31)(H,29,32)/b22-13-. InChi Key: INQUULPXCZAKMS-XKZIYDEJSA-N.