2. PI3K/Akt/mTOR
  3. Akt
  4. BAY1125976

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.

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

BAY1125976 Chemical Structure

BAY1125976 Chemical Structure

CAS No. : 1402608-02-9

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Solid + Solvent
10 mM * 1 mL in DMSO
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2 mg USD 60 In-stock
5 mg USD 100 In-stock
10 mg USD 170 In-stock
50 mg USD 560 In-stock
100 mg USD 900 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

BAY1125976 Related Antibodies

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Akt Akt1 Akt2 Akt3

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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.

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)

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.

BAY1125976 Related Antibodies
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].

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

383.45

Formula

C23H21N5O
CAS No.
Appearance

Solid

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
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6079 mL 13.0395 mL 26.0790 mL
5 mM 0.5216 mL 2.6079 mL 5.2158 mL
View the Complete Stock Solution Preparation Table

* 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

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
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].

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].

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

Complete Stock Solution Preparation Table

* 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.

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
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BAY1125976 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BAY11259761402608-02-9BAY 1125976BAY-1125976AktPKBProtein kinase BInhibitorinhibitorinhibit

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