WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407996
Description: BAY-1125976 is a potent and selective allosteric AKT1/2 inhibitor. BAY-1125976 exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models. BAY 1125976 potently and selectively inhibited the activity of full-length AKT1 and AKT2 by binding into an allosteric binding pocket formed by kinase and PH domain. In vitro, BAY 1125976 inhibited cell proliferation in a broad panel of human cancer cell lines. BAY 1125976 exhibited 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.
MedKoo Cat#: 407996
Chemical Formula: C23H21N5O
Exact Mass: 383.1746
Molecular Weight: 383.45
Elemental Analysis: C, 72.04; H, 5.52; N, 18.26; O, 4.17
Synonym: BAY-1125976; BAY 1125976; BAY1125976;
IUPAC/Chemical Name: Imidazo[1,2-b]pyridazine-6-carboxamide, 2-[4-(1-aminocyclobutyl)phenyl]-3-phenyl-
InChi Key: JBGYKRAZYDNCNV-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: O=C(C1=NN2C(C=C1)=NC(C3=CC=C(C4(N)CCC4)C=C3)=C2C5=CC=CC=C5)N
The PI3K-AKT-mTOR signaling cascade is activated in the majority of human cancers, and its activation also plays a key role in resistance to chemo and targeted therapeutics. In particular, in both breast and prostate cancer, increased AKT pathway activity is associated with cancer progression, treatment resistance and poor disease outcome.
1: Politz O, Siegel F, Bärfacker L, Bömer U, Hägebarth A, Scott WJ, Michels M,
Ince S, Neuhaus R, Meyer K, Fernández-Montalván AE, Liu N, von Nussbaum F,
Mumberg D, Ziegelbauer K. 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. Epub 2016 Oct
20. PubMed PMID: 27699769.