BAY 1125976
SIGMA/SML2842 - ≥98% (HPLC)
Synonym: 2-
CAS Number: 1402608-02-9
Empirical Formula (Hill Notation): C23H21N5O
Molecular Weight: 383.45
MDL Number: MFCD30481340
Linear Formula: C23H21N5O
Product Type: Chemical
| assay | ≥98% (HPLC) |
| color | white to beige |
| form | powder |
| Quality Level | 100  |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | 2-8°C |
| 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. |
| WGK Germany | WGK 3 |
| Flash Point(F) | Not applicable |
| Flash Point(C) | Not applicable |
| Purity | ≥98% (HPLC) |
| Storage Temp. | 2-8°C |
| UNSPSC | 12352200 |