BAY-1125976.
- Product Name
- BAY-1125976.
- CAS No.
- 1402608-02-9
- Chemical Name
- BAY-1125976.
- Synonyms
- CS-2913;BAY1125976;BAY 1125976;BAY-1125976.;BAY-1125976; BAY 1125976;BAY1125976, 10 mM in DMSO;inhibit,Inhibitor,Protein kinase B,Akt,BAY 1125976,BAY1125976,PKB,BAY-1125976;2-[4-(1-Aminocyclobutyl)phenyl]-3-phenylimidazo[1,2-b]pyridazine-6-carboxamide;Imidazo[1,2-b]pyridazine-6-carboxamide, 2-[4-(1-aminocyclobutyl)phenyl]-3-phenyl-
- CBNumber
- CB73133467
- Molecular Formula
- C23H21N5O
- Formula Weight
- 383.45
- MOL File
- 1402608-02-9.mol
BAY-1125976. Property
- storage temp.
- Store at -20°C
- solubility
- DMSO:13.0(Max Conc. mg/mL);33.9(Max Conc. mM)
DMF:5.0(Max Conc. mg/mL);13.04(Max Conc. mM)
DMF:PBS (pH 7.2) (1:3):0.25(Max Conc. mg/mL);0.65(Max Conc. mM) - form
- A crystalline solid
- color
- Light yellow to yellow
N-Bromosuccinimide Price
- Product number
- 28913
- Product name
- BAY-1125976
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 28913
- Product name
- BAY-1125976
- Packaging
- 25mg
- Price
- $533
- Updated
- 2024/03/01
- Product number
- 28913
- Product name
- BAY-1125976
- Packaging
- 5mg
- Price
- $139
- Updated
- 2024/03/01
- Product number
- 28913
- Product name
- BAY-1125976
- Packaging
- 10mg
- Price
- $243
- Updated
- 2024/03/01
- Product number
- 2002DU
- Product name
- 2-[4-(1-Aminocyclobutyl)phenyl]-3-phenylimidazo[1,2-b]pyridazine-6-carboxamide
- Packaging
- 5mg
- Price
- $252
- Updated
- 2021/12/16
BAY-1125976. Chemical Properties,Usage,Production
Description
BAY-1125976 is an allosteric inhibitor of Akt1 and -2 (IC50s = 5.2 and 18 nM, respectively, in a time-resolved FRET assay). It is selective for Akt1 and -2 over Akt3 (IC50 = 427 nM in the same assay) but does inhibit the activity of the receptor tyrosine kinases FLT1, -3, -4, and Mer by greater than 50% in a panel of 227 kinases at 1 μM. BAY-1125976 inhibits the proliferation of 23 cancer cell lines (IC50s = 0.02-10 μM) and reduces tumor growth in KPL-4, MCF-7, and patient-derived xenograft (PDX) mouse models when administered at a dose of 50 mg/kg per day.
Uses
BAY1125976 is a selective allosteric Akt1/Akt2 inhibitor; inhibits Akt1 and Akt2 activity with IC50 values of 5.2 nM and 18 nM at 10 μM ATP, respectively.
in vivo
BAY 1125976 targets tumors displaying activation of the PI3K/Akt/mTOR pathway. BAY 1125976 exhibits strong in vivo efficacy in both cell line and patient-derived xenograft models such as the KPL4 breast cancer model (PIK3CAH1074R mutant), the MCF7 and HBCx-2 breast cancer models, and the AktE17K mutant driven prostate cancer (LAPC-4) and anal cancer (AXF 984) models[1].
IC 50
Akt1: 5.2 nM (IC50, at 10 μM ATP); Akt2: 18 nM (IC50, at 10 μM ATP); Akt3: 427 nM (IC50, at 10 μM ATP)
References
[1] Politz O, et al. BAY 1125976, a selective allosteric AKT1/2 inhibitor, exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models. Int J Cancer. 2017 Jan 15;140(2):449-459. DOI:10.1002/ijc.30457
BAY-1125976. Preparation Products And Raw materials
Raw materials
Preparation Products
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