SML2943

LY2409881 hydrochloride

≥98% (HPLC)

• Synonyme(s) : 2-{5-Chloro-2-[3-(4-methylpiperazin-1-yl)propylamino]-pyrimidin-4-yl}benzo[b]thiophene-4-carboxylic acid cyclopropylamide hydrochloride, LY 2409881 hydrochloride, LY-2409881 hydrochloride, N-Cyclopropyl-2-[5-Chloro-2-[[3-(4-methylpiperazin-1-yl)propyl]amino]pyrimidin-4-yl]benzo[b]thiophene-4-carboxamide hydrochloride
• Formule empirique (notation de Hill): C₂₄H₂₉ClN₆OS · xHCl
• Poids moléculaire : 485.04 (free base basis)
• Numéro MDL: MFCD28900675
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Essai: ≥98% (HPLC)
• Forme: powder
• Conditions de stockage: desiccated
• Couleur: white to beige
• Solubilité: H₂O: 2 mg/mL, clear
• Température de stockage: −20°C

Description

Actions biochimiques/physiologiques

LY2409881 is a potent IκΒ kinase β (IKK2, IKKβ, IKKbeta) inhibitor (IC50 = 30 nM) that effectively inhibits 10 ng/mL TNFα-induced IκB phosphorylation in LY10 DLBCL cells (by >95%; 10 μM) and exhibits good selectivity by kinase profiling among more than 300 kinases (>10-fold selectivity). LY2409881 enhances TNFα cytotoxicity in SKOV3 ovarian cancer cultures (~20% survival with 316 nM LY2409881 & 10 ng/mL TNFα in 72 hrs; 100% survival with LY2409881 or TNFα alone) by blocking NF-κB antiapoptotic signal activation without affecting TRADD & FADD proapoptotic pathway induction. When administered in vivo, LY2409881 is shown to suppress LY10 xenograft-derived tumor growth in mice (50-200 mg/kg, twice weekly ip.).

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable