SML1679

DEL-22379

≥98% (HPLC)

• Synonym(s): N-(3-((5-Methoxy-1H-indol-3-yl)methylene)-2-oxoindolin-5-yl)-3-(piperidin-1-yl)propanamide, N-[2,3-Dihydro-3-[(5-methoxy-1H-indol-3-yl)methylene]-2-oxo-1H-indol-5-yl]-1-piperidinepropanamide
• Empirical Formula (Hill Notation): C₂₆H₂₈N₄O₃
• CAS Number: 181223-80-3
• Molecular Weight: 444.53
• MDL number: MFCD00950163
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 10 mg/mL, clear
• storage temp.: −20°C
• SMILES string: O=C1NC2=CC=C(NC(CCN3CCCCC3)=O)C=C2C1=CC4=CNC5=C4C=C(OC)C=C5
• InChI key: INQUULPXCZAKMS-UHFFFAOYSA-N

Description

Biochem/physiol Actions

DEL-22379 is a cell-permeable 3-arylidene-2-oxindole derivative that inhibits the dimerization of ERK (IC₅₀ = 500 nM) via directly binding to its dimerization interface. DEL-22379 promotes the transactivation of ELK, and prevents the EGF-induced phosphorylation of the cytoplasmic kinase RSK1 in HEK293 cells (IC₅₀ = 500 nM). DEL-22379 induces apoptosis in various cancer cells harboring RAS-ERK pathway oncogenes (IC₅₀ = 150 – 400 nM). DEL-22379 blocks tumor progression and metastasis in multiple xenograft models such as A375 (BRAF mutant), HCT116 (KRAS mutant) and colorectal cancer patient-derived xenografts (15 mg/kg, i.p. b.i.d.).

DEL-22379 is a cell-permeable 3-arylidene-2-oxindole derivative that inhibits the dimerization of ERK via directly binding to its dimerization interface.

Safety Information

• Pictograms: GHS07
• Signal Word: Warning
• Hazard Statements: H315,H319
• Precautionary Statements: P264 - P280 - P302 + P352 - P305 + P351 + P338 - P332 + P313 - P337 + P313
• Hazard Classifications: Eye Irrit. 2 - Skin Irrit. 2
• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable