| Literature DB >> 22819764 |
Sonia Martínez González1, Ana Isabel Hernández, Carmen Varela, Milagros Lorenzo, Francisco Ramos-Lima, Elena Cendón, David Cebrián, Enara Aguirre, Elena Gomez-Casero, M I Albarrán, Patricia Alfonso, Beatriz García-Serelde, Genoveva Mateos, Julen Oyarzabal, Obdulia Rabal, Francisca Mulero, Teresa Gonzalez-Granda, Wolfgang Link, Jesús Fominaya, Mariano Barbacid, James R Bischoff, Pilar Pizcueta, Carmen Blanco-Aparicio, Joaquín Pastor.
Abstract
Phosphoinositide-3-kinases (PI3K) are a family of lipid kinases mediating numerous cell processes such as proliferation, migration and differentiation. PI3K is an important target for cancer therapeutics due to the deregulation of this signaling pathway in a wide variety of human cancers. Herein, we describe the rapid identification of ETP-46992, within 2-aminocarbonyl imidazo [1,2-a] pyrazine series, with suitable pharmacokinetic (PK) properties that allows the establishment of mechanism of action and efficacy in vivo studies. ETP-46992 showed tumor growth inhibition in a GEMM mouse tumor model driven by a K-Ras(G12V) oncogenic mutation and in tumor xenograft models with PI3K pathway deregulated (BT474).Entities:
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Year: 2012 PMID： 22819764 DOI： 10.1016/j.bmcl.2012.06.093
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823