BAY-1125976. Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMSO:13.0(Max Conc. mg/mL);33.9(Max Conc. mM)
DMF:5.0(Max Conc. mg/mL);13.04(Max Conc. mM)
DMF:PBS (pH 7.2) (1:3):0.25(Max Conc. mg/mL);0.65(Max Conc. mM)

form 

A crystalline solid

color 

Light yellow to yellow

InChI

InChI=1S/C23H21N5O/c24-22(29)18-11-12-19-26-20(21(28(19)27-18)16-5-2-1-3-6-16)15-7-9-17(10-8-15)23(25)13-4-14-23/h1-3,5-12H,4,13-14,25H2,(H2,24,29)

InChIKey

JBGYKRAZYDNCNV-UHFFFAOYSA-N

SMILES

C12=NC(C3=CC=C(C4(N)CCC4)C=C3)=C(C3=CC=CC=C3)N1N=C(C(N)=O)C=C2

BAY-1125976. Usage And Synthesis

Description

BAY-1125976 is an allosteric inhibitor of Akt1 and -2 (IC₅₀s = 5.2 and 18 nM, respectively, in a time-resolved FRET assay). It is selective for Akt1 and -2 over Akt3 (IC₅₀ = 427 nM in the same assay) but does inhibit the activity of the receptor tyrosine kinases FLT1, -3, -4, and Mer by greater than 50% in a panel of 227 kinases at 1 μM. BAY-1125976 inhibits the proliferation of 23 cancer cell lines (IC₅₀s = 0.02-10 μM) and reduces tumor growth in KPL-4, MCF-7, and patient-derived xenograft (PDX) mouse models when administered at a dose of 50 mg/kg per day.

Uses

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.

in vivo

IC 50

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)

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. DOI:10.1002/ijc.30457

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