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Ref Type
Authors Oliver Politz, Arne Scholz, Andrea Haegebarth, Ningshu Liu, Lars Baerfacker, Stuart Ince, Roland Neuhaus, Ulf Boemer, Martin Michels, and Dominik Mumberg
Title Abstract 3685: BAY 1125976, is a selective allosteric AKT1/2 inhibitor with high efficacy in AKT1-mutated cancers
Journal Cancer Res
Vol 34
Date October 1
Abstract Text doi: 10.1158/1538-7445.AM2014-3685 Cancer Res October 1, 2014 74; 3685


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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
BAY1125976 BAY1125976 11 1
Drug Name Trade Name Synonyms Drug Classes Drug Description
BAY1125976 BAY 1125976 Akt1 Inhibitor 6 Akt2 Inhibitor 2 BAY1125976 inhibits the activity of AKT1/2, which may result in reduced tumor cell proliferation and decreased growth of tumors with activated PI3K/AKT/mTOR signaling (PMID: 27699769).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
AKT1 E17K anal canal cancer sensitive BAY1125976 Preclinical - Pdx Actionable In a preclinical study, treatment with BAY1125976 reduced tumor growth and resulted in partial tumor regression or stable disease in anal cancer patient-derived xenograft (PDX) models harboring AKT1 E17K (PMID: 27699769). 27699769 detail...
AKT1 E17K NRAS Q61R bladder carcinoma sensitive BAY1125976 Preclinical - Cell culture Actionable In a preclinical study, BAY1125976 inhibited Akt activation and downstream signaling in bladder cancer cell lines carrying both Akt1 E17K and Nras Q61R mutations (AACR; Cancer Res 2014;74(19 Suppl):Abstract nr 3685). detail...