SML4098

RO4929097

≥98% (HPLC)

• Synonym(s): 2,2-Dimethyl-N-((S)-6-oxo-6,7-dihydro-5H-dibenzo[b, d]azepin-7-yl)-N′-(2,2,3,3,3-pentafluoro-propyl)-malonamide, N1-[(7S)-6,7-Dihydro-6-oxo-5H-dibenz[b,d]azepin-7-yl]-2,2-dimethyl-N3-(2,2,3,3,3-pentafluoropropyl)propanediamide, RO 4929097, RO-4929097
• Empirical Formula (Hill Notation): C₂₂H₂₀F₅N₃O₃
• CAS Number: 847925-91-1
• Molecular Weight: 469.40
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: -10 to -25°C

Description

Biochem/physiol Actions

Orally active, potent and selective gamma-secretase inhibitor with anti-cancer efficacy in vitro and in vivo.

RO4929097 is an orally active, potent and selective gamma-secretase (γ-secretase) inhibitor (IC50 = 4 nM) that blocks Aβ1-40 production (IC50 = 14 nM in APP-overexpressing HEK293) and suppresses Notch signaling (IC50 = 5 nM by reporter assays) with >100-fold selectivity over 75 other enzymes, receptors and ion channels. RO4929097 reduces the size of MDA-MB-468 soft agar colonies in cultures (100-250 nM) and effectively suppresses A549 NSCLC xenografts-derived tumor growth in mice in vivo (3-60 mg/kg bid or qd p.o.).