Home PI3K/Akt/mTOR Akt inhibitor BAY1125976 For research use only.

BAY1125976

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).

BAY1125976 Chemical Structure

BAY1125976 Chemical Structure

CAS: 1402608-02-9

Purity & Quality Control

Batch: Purity: 99.89%
99.89

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Description 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).
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
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
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/Cvolume 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/Cvolume values of 0.25 and 0.25 and T/Cweight values of 0.33 and 0.37, respectively. BAY 1125976 displays good antitumor efficacy in vivo in AKT1E17K mutated models.[1].
Animal Research Animal Models Female 5-7 week old NMRI nude (nu/nu) mice, Male 8-10 week old SCID (scid/scid) mice, Female athymic nude Foxn1nu mice, Female 5-week-old Foxn1nu nude (nu/nu) mice
Dosages 5, 10, 15, 25, 50 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01915576 Completed Neoplasms Bayer September 2013 Phase 1

Chemical lnformation & Solubility

Molecular Weight 383.45 Formula

C23H21N5O

 
CAS No. 1402608-02-9 SDF --
Smiles C1CC(C1)(C2=CC=C(C=C2)C3=C(N4C(=N3)C=CC(=N4)C(=O)N)C5=CC=CC=C5)N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 11 mg/mL ( (28.68 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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