Cat. No.: HY-100018

BAY1125976

3 Cited Publications

Customer Review

Based on 3 publication(s) in Google Scholar

BAY1125976, a chemical probe, 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.

For research use only. We do not sell to patients.

Purity: 99.52%
CAS No.: 1402608-02-9
Formula: C₂₃H₂₁N₅O
Molecular Weight:383.45

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

BAY1125976 Chemical Structure

CAS No.: 1402608-02-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

BAY1125976, a chemical probe, 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.

IC₅₀ & Target^[1]

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)

All Akt Isoforms :

In Vitro

BAY 1125976 is equally potent against Akt1 (IC₅₀=5.2 nM at 10 μM ATP and 44 nM at 2 mM ATP) and Akt2 (IC₅₀=18 nM at 10 μM ATP and 36 nM at 2 mM ATP) isoforms and up to 86 fold less potent against Akt3 (IC₅₀=427 nM at 10 μM ATP). It inhibits the Akt1 and Akt2 by binding into an allosteric binding pocket formed by kinase and PH domain. It inhibits cell proliferation in a broad panel of human cancer cell lines, particularly in breast and prostate cancer cell lines expressing estrogen or androgen receptors. It effectively blocks Akt signaling by inhibiting the phosphorylation of Akt and the downstream effectors, including eukaryotic translation initiation factor 4E binding protein 1 (4E-BP1), glycogen synthase kinase 3 beta (GSK3s), proline-rich Akt substrate 40 kDa (PRAS40), S6 ribosomal protein (S6RP), and 70 kDa ribosomal protein S6 kinase 1 (70S6K)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 (PIK3CA^H1074R mutant), the MCF7 and HBCx-2 breast cancer models, and the Akt^E17K mutant driven prostate cancer (LAPC-4) and anal cancer (AXF 984) models^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1402608-02-9
Appearance Solid
Molecular Weight 383.45
Formula C₂₃H₂₁N₅O
Color Light yellow to yellow
SMILES

O=C(C1=NN2C(C=C1)=NC(C3=CC=C(C4(N)CCC4)C=C3)=C2C5=CC=CC=C5)N
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (3)

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Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Sci Rep

Network analysis of gene expression reveals regulators of cell viscosity and mechanical phenotype. [Abstract]

2025 Sep 30;15(1):34008. PMID: 41028875
bioRxiv

2024 May 24.

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (65.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6079 mL

13.0395 mL

26.0790 mL

5 mM

0.5216 mL

2.6079 mL

5.2158 mL

10 mM

0.2608 mL

1.3040 mL

2.6079 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Kinase Assay^[1]

PEG/water (60/40), pH 4.0, is used as a vehicle for BAY 1125976. The selectivity of BAY 1125976 is assessed using two different kinase panels: the 230 kinase panel; and the 468 kinase panel. In the 230 kinase panel, kinase activity is determined after incubation with 10 μM BAY 1125976. An additional incubation with 1 μM and 0.1 μM BAY 1125976 is performed for the kinases where 10 μM BAY 1125976 shows an inhibition over 70%. All tests are performed at 10 μM ATP. The 468-kinase panel covered AGC, CAMK, CMGC, CK1, STE, TK, TKL, lipid, and atypical kinase families. The profiling is performed by combining the test compound with DNA-tagged kinase and immobilized ligands. The final kinase concentrations are measured by quantitative PCR^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice: Female NMRI (nu/nu) mice s.c. injected with 3 x 10⁶/100 μL KPL-4 breast cancer cells are used to study the mode-of-action of BAY 1125976. The treatment is started when tumors reaches 232-358 mm³ in size and the mice receive a single oral dose of 25 or 50 mg/kg BAY 1125976. For determination of plasma concentration-time profiles, blood is drawn from the animals at different time points after compound administration^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6079 mL	13.0395 mL	26.0790 mL	65.1975 mL
	5 mM	0.5216 mL	2.6079 mL	5.2158 mL	13.0395 mL
	10 mM	0.2608 mL	1.3040 mL	2.6079 mL	6.5198 mL
	15 mM	0.1739 mL	0.8693 mL	1.7386 mL	4.3465 mL
	20 mM	0.1304 mL	0.6520 mL	1.3040 mL	3.2599 mL
	25 mM	0.1043 mL	0.5216 mL	1.0432 mL	2.6079 mL
	30 mM	0.0869 mL	0.4347 mL	0.8693 mL	2.1733 mL
	40 mM	0.0652 mL	0.3260 mL	0.6520 mL	1.6299 mL
	50 mM	0.0522 mL	0.2608 mL	0.5216 mL	1.3040 mL
	60 mM	0.0435 mL	0.2173 mL	0.4347 mL	1.0866 mL

Keywords

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BAY1125976

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Chemical Probe Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) BAY1125976

All Akt Isoforms

Biological Activity

Chemical Information

Publications (3)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

BAY1125976 Related Classifications

Cat. No.: HY-100018