SML2842

BAY 1125976

≥98% (HPLC)

• Synonym(e): 2-[4-(1-Aminocyclobutyl)phenyl]-3-phenylimidazo[1,2-b]pyridazine-6-carboxamide, BAY-1125976, BAY1125976
• Empirische Formel (Hill-System): C₂₃H₂₁N₅O
• CAS-Nummer: 1402608-02-9
• Molekulargewicht: 383.45
• MDL-Nummer: MFCD30481340
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: 2-8°C

Beschreibung

Biochem./physiol. Wirkung

BAY 1125976 is an orally active, potent and highly selective AKT1/2 allosteric inhibitor (IC₅₀ = 5.2/18 nM with 10 μM ATP, IC₅₀ = 44/36 nM with 2 mM ATP; AKT3 IC₅₀ = 427 nM with 10 μM ATP) that targets a pocket formed by the kinase & PH domain. BAY 1125976 reduces basal AKT T308/S473 phosphorylation (IC₅₀ = 0.9/1.1; KPL-4 cells) and exhibits anti-cancer efficacy in cultures (IC₅₀ = 0.02-10 μM, 23 human cancer lines) and in xenograft models in vivo (25, 50 mg/kg/day or 5, 15, 25 mg/kg bid. po.; mice), including breast cancers (KPL4 PIK3CAH1074R mutant, MCF7, HBCx-2), AKTE17K-driven prostate cancer LAPC-4, and anal cancer AXF 984.

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable