کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1371249 | 981841 | 2012 | 7 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR](/preview/png/1371249.png)
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-RasG12V oncogenic mutation and in tumor xenograft models with PI3K pathway deregulated (BT474).
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Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 16, 15 August 2012, Pages 5208–5214