1253573-53-3

Usage

Uses

Used in Cancer Therapeutics:
AMG 511 is used as a cancer therapeutic agent for its effect on cell growth and cell survival. It specifically targets the PI3Kα pathway, which is often dysregulated in various types of cancer, leading to uncontrolled cell proliferation and resistance to apoptosis. By inhibiting this pathway, AMG 511 can potentially halt tumor growth and improve patient outcomes.
Used in Oncology Research:
In addition to its therapeutic applications, AMG 511 can also be utilized in oncology research to better understand the role of the PI3Kα pathway in cancer development and progression. This knowledge can help researchers identify new targets for cancer treatment and develop more effective strategies for combating the disease.
Used in Drug Development:
AMG 511 serves as a valuable compound in the development of new drugs targeting the PI3Kα pathway. Its success in inhibiting this pathway can guide the design and synthesis of novel compounds with improved efficacy, selectivity, and safety profiles, ultimately leading to more effective cancer treatments.

Upstream product

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• 1253571-14-0 5-(4-(bis(4-methoxybenzyl)-amino)-6-methyl-1,3,5-triazin-2-yl)-6-((5-fluoro-6-methoxypyridin-3-yl)amino)nicotinaldehyde 
• 1253571-15-1 1-(5-(4-(bis(4-methoxybenzyl)amino)-6-methyl-1,3,5-triazin-2-yl)-6-((5-fluoro-6-methoxypyridin-3-yl)amino)pyridin-3-yl)ethanol 
• 1253575-95-9 1-(5-(4-(bis(4-methoxybenzyl)amino)-6-methyl-1,3,5-triazin-2-yl)-6-((5-fluoro-6-methoxypyridin-3-yl)amino)pyridin-3-yl)ethyl methanesulfonate 
• 1253571-16-2 4-(2-((5-fluoro-6-methoxypyridin-3-yl)amino)-5-(1-(4-(methylsulfonyl)piperazin-1-yl)ethyl)pyridin-3-yl)-N,N-bis(4-methoxybenzyl)-6-methyl-1,3,5-triazin-2-amine 
• 1253575-94-8 4-(5-chloro-2-((5-fluoro-6-methoxypyridin-3-yl)amino)pyridin-3-yl)-N,N-bis(4-methoxybenzyl)-6-methyl-1,3,5-triazin-2-amine 
• 1253571-12-8 4-(5-(1,3-dioxolan-2-yl)-2-fluoropyridin-3-yl)-N,N-bis-(4-methoxybenzyl)-6-methyl-1,3,5-triazin-2-amine 
• 886372-63-0 5-fluoro-6-methoxypyridin-3-ylamine 
• 1253575-93-7 1-(5-(4-(bis(4-methoxybenzyl)amino)-6-methyl-1,3,5-triazin-2-yl)-6-((5-fluoro-6-methoxypyridin-3-yl)amino)pyridin-3-yl)ethanone 
• 1253573-54-4 (R)-N,N-bis(4-methoxybenzyl)-4-(2-(5-fluoro-6-methoxypyridin-3-ylamino)-5-(1-(4-(methylsulfonyl)piperazin-1-yl)ethyl)pyridin-3-yl)-6-methyl-1,3,5-triazin-2-amine 
• 1253571-11-7 4-(2-((5-fluoro-6-methoxypyridin-3-yl)amino)-5-(1-(4-(methylsulfonyl)piperazin-1-yl)ethyl)pyridin-3-yl)-6-methyl-1,3,5-triazin-2-amine 

Relevant academic research and scientific papers

Selective class i phosphoinositide 3-kinase inhibitors: Optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511

The phosphoinositide 3-kinase family catalyzes the phosphorylation of phosphatidylinositol-4,5-diphosphate to phosphatidylinositol-3,4,5-triphosphate, a secondary messenger which plays a critical role in important cellular functions such as metabolism, cell growth, and cell survival. Our efforts to identify potent, efficacious, and orally available phosphatidylinositol 3-kinase (PI3K) inhibitors as potential cancer therapeutics have resulted in the discovery of 4-(2-((6-methoxypyridin-3-yl)amino)-5-((4-(methylsulfonyl) piperazin-1-yl)methyl)pyridin-3-yl)-6-methyl-1,3,5-triazin-2-amine (1). In this paper, we describe the optimization of compound 1, which led to the design and synthesis of pyridyltriazine 31, a potent pan inhibitor of class I PI3Ks with a superior pharmacokinetic profile. Compound 31 was shown to potently block the targeted PI3K pathway in a mouse liver pharmacodynamic model and inhibit tumor growth in a U87 malignant glioma glioblastoma xenograft model. On the basis of its excellent in vivo efficacy and pharmacokinetic profile, compound 31 was selected for further evaluation as a clinical candidate and was designated AMG 511.

INHIBITORS OF PI3 KINASE AND / OR MTOR

The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.