BAY 1125976 (C005B-310016)

Catalog No.: C005B-310016
Manufacturer No.: SML2842-5MG
Manufacturer Name: Sigma-Aldrich
Quantity: 5
Unit of Measure: MG

Biochem/physiol Actions BAY 1125976 is an orally active, potent and highly selective AKT1/2 allosteric inhibitor (IC 50 = 5.2/18 nM with 10 μ:M ATP, IC 50 = 44/36 nM with 2 mM ATP: AKT3 IC 50 = 427 nM with 10 μ:M ATP) that targets a

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Description
Specifications

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.

UPC:: 42191610
Condition:: New
HazmatClass:: No
MPN:: SML2842-5MG
CAS:: 1402608-02-9

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