BAY1125976

Name: BAY1125976
Brand: Selleck Chemicals
SKU: S8500
Rating: 5 (0 reviews)

For research use only.

Catalog No.S8500

CAS No. 1402608-02-9

BAY 1125976 is a selective allosteric AKT1/2 inhibitor,exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models. BAY1125976 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 BAY1125976 is almost inactive on AKT3 (IC50 = 427 nM at 10 µM ATP).

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Biological Activity

Description

Targets

Akt1 ^[1] (at 10 µM ATP)	Akt2 ^[1] (at 10 µM ATP)	Akt2 ^[1] (at 2 mM ATP)	Akt1 ^[1] (at 2 mM ATP)	Akt3 ^[1] (at 10 µM ATP)
5.2 nM	18 nM	36 nM	44 nM	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 BAY 1125976 results in an inhibition of PRAS40 phosphorylation at T246 as a direct target of AKT1 activity with an IC50 of ∼141 nM. BAY 1125976 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 BAY 1125976 treatment.^[1].

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 BAY 1125976 with T/C_volume ratios of 0.14 and 0.08, respectively. Daily administration of 25 or 50 mg/kg BAY 1125976 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. BAY 1125976 displays good antitumor efficacy in vivo in AKT1^E17K mutated models.^[1].

Protocol

Animal Research: ^[1]	- Collapse Animal Models: Female 5-7 week old NMRI nude (nu/nu) mice, Male 8-10 week old SCID (scid/scid) mice, Female athymic nude Foxn1^nu mice, Female 5-week-old Foxn1^nu nude (nu/nu) mice Dosages: 5, 10, 15, 25, 50 mg/kg Administration: Oral gavage (Only for Reference)

References

[1] Politz O, et al. Int J Cancer. 2017 Jan 15;140(2):449-459.

Solubility (25°C)

In vitro	DMSO	11 mg/mL (28.68 mM)
	Water	Insoluble
	Ethanol	Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight	383.45
Formula	C₂₃H₂₁N₅O
CAS No.	1402608-02-9
Storage	3 years-20°C powder 2 years-80°C in 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

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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.

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-05-17)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01915576	Completed	Drug: BAY1125976	Neoplasms	Bayer	September 2013	Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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