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BAY1125976 Akt inhibitor

Name: BAY1125976
Brand: Selleck Chemicals
SKU: S8500
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S8500

BAY 1125976 is a selective allosteric AKT1/2 inhibitor, exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models. This compound inhibits the activity of 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) very potently. Whereas this chemical is almost inactive on AKT3 (IC50 = 427 nM at 10 µM ATP).

Chemical Structure

Molecular Weight: 383.45

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Quality Control

Batch: Purity: 99.89%

99.89

Related Targets	PI3K mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
Other Akt Products	MK-2206 Dihydrochloride SC79 AZD5363 (Capivasertib) Ipatasertib (GDC-0068) Perifosine GSK690693 Triciribine (API-2) CCT128930 Afuresertib (GSK2110183) A-674563 HCl

Solubility

In vitro
Batch:

DMSO : 11 mg/mL (28.68 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.550mg/ml (1.43mM)	Taking the 1 mL working solution as an example, add 50 μL of 11 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.260mg/ml (0.68mM)	Taking the 1 mL working solution as an example, add 50 μL of 5.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	383.45	Formula	C₂₃H₂₁N₅O	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1402608-02-9	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CC(C1)(C2=CC=C(C=C2)C3=C(N4C(=N3)C=CC(=N4)C(=O)N)C5=CC=CC=C5)N

Mechanism of Action

Targets/IC₅₀/Ki	Akt1 (at 10 µM ATP) 5.2 nM Akt2 (at 10 µM ATP) 18 nM Akt2 (at 2 mM ATP) 36 nM Akt1 (at 2 mM ATP) 44 nM Akt3 (at 10 µM ATP) 427 nM
In vitro	BAY 1125976 inhibits activation of AKT in cell lines carrying the AKT-activating mutation E17K. In KU-19-19 bladder cancer cells activation by phosphorylation is inhibited at AKT1-S473 and 4EBPI-T70 with IC50 values of 35 and 100 nM, respectively. In the prostate cancer cell line LAPC-4, the phosphorylation of AKT1-S473, T308 and 4EBP1-T70 is inhibited with IC50 values of 0.8, 5.6 and 35 nM, respectively. Treatment of LAPC-4 cells with this compound results in an inhibition of PRAS40 phosphorylation at T246 as a direct target of AKT1 activity with an IC50 of ∼141 nM. This chemical inhibits the proliferation of the breast cancer cell lines BT-474, T47D, MCF7, ZR-75–1, EVSA-T, MDA-MB-453, KPL-4 and BT20 as well as the prostate cancer cell lines LNCaP and LAPC-4 with submicromolar IC50 values. Breast cancer cell lines of luminal type show strong inhibition of cell proliferation following this compound treatment..
In vivo	Treatment with different doses of BAY 1125976 results in potent antitumor efficacy in KPL-4 tumor bearing mice. A clear, statistically significant dose-response is observed after daily oral treatment with 25 or 50 mg/kg of this compound with T/C_volume ratios of 0.14 and 0.08, respectively. Daily administration of 25 or 50 mg/kg of this chemical results in significant antitumor efficacy in MCF7-implanted nude mice compared with the control with T/C_volume values of 0.25 and 0.25 and T/C_weight values of 0.33 and 0.37, respectively. This compound displays good antitumor efficacy in vivo in AKT1^E17K mutated models..
References	[1] https://pubmed.ncbi.nlm.nih.gov/27699769/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01915576	Completed	Neoplasms	Bayer	September 2013	Phase 1

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