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Updated: Jan 3, 2026

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
Published on: October 23, 2019
Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors
Christoph M Dehnhardt1, Aranapakam M Venkatesan, Zecheng Chen
1Medicinal Chemistry, Pfizer, 401 N. Middletown Rd., Pearl River, NY 10965, USA. christoph.dehnhardt@pfizer.com
Abstract:
We recently described several highly potent, triazine (1) and triazolopyrimidine (2) scaffold-based, dual PI3K/mTOR-inhibitors (e.g., 1, PKI-587) that were efficacious in both in vitro and in vivo models. In order to further optimize these compounds we devised a novel series, the 2-oxatriazines, which also exhibited excellent potency and good metabolic stability. Some 2-oxatriazines showed promising in vivo biomarker suppression and induced apoptosis in the MDA-MB-361 breast cancer xenograft model.
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