1197165-80-2

Upstream product

• 6601-22-5 2,6-Dichloro-4-morpholino-1,3,5-triazine 
• 32315-10-9 bis(trichloromethyl) carbonate 
• 55121-99-8 (4-aminophenyl)(4-methylpiperazin-1-yl)methanone 
• 1332327-20-4 C₁₆H₁₉N₅O₃ 
• 1332327-22-6 C₁₀H₁₃ClN₄O₃ 

Relevant academic research and scientific papers

Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors

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.

TRIAZINE COMPOUNDS AS PI3 KINASE AND MTOR INHIBITORS

Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.