SML2842

BAY 1125976

≥98% (HPLC)

• Sinónimos: 2-[4-(1-Aminocyclobutyl)phenyl]-3-phenylimidazo[1,2-b]pyridazine-6-carboxamide, BAY-1125976, BAY1125976
• Fórmula empírica (notación de Hill): C₂₃H₂₁N₅O
• Número de CAS: 1402608-02-9
• Peso molecular: 383.45
• MDL number: MFCD30481340
• UNSPSC Code: 12352200
• NACRES: NA.77

Propiedades

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C

Descripción

Biochem/physiol Actions

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.

Información de seguridad

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable