In 2022,Fairhurst, Robin A.; Furet, Pascal; Imbach-Weese, Patricia; Stauffer, Frederic; Rueeger, Heinrich; McCarthy, Clive; Ripoche, Sebastien; Oswald, Susanne; Arnaud, Bertrand; Jary, Aline; Maira, Michel; Schnell, Christian; Guthy, Daniel A.; Wartmann, Markus; Kiffe, Michael; Desrayaud, Sandrine; Blasco, Francesca; Widmer, Toni; Seiler, Frank; Gutmann, Sascha; Knapp, Mark; Caravatti, Giorgio published an article in Journal of Medicinal Chemistry. The title of the article was 《Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor》.Quality Control of 2,4,6-Trichloropyrimidine The author mentioned the following in the article:
Balanced pan-class I phosphoinositide 3-kinase inhibition as an approach to cancer treatment offers the prospect of treating a broad range of tumor types and/or a way to achieve greater efficacy with a single inhibitor. Taking buparlisib as the starting point, the balanced pan-class I PI3K inhibitor 40 (NVP-CLR457) was identified with what was considered to be a best-in-class profile. Key to the optimization to achieve this profile was eliminating a microtubule stabilizing off-target activity, balancing the pan-class I PI3K inhibition profile, minimizing CNS penetration, and developing an amorphous solid dispersion formulation. A rationale for the poor tolerability profile of 40 in a clin. study is discussed. The experimental process involved the reaction of 2,4,6-Trichloropyrimidine(cas: 3764-01-0Quality Control of 2,4,6-Trichloropyrimidine)
2,4,6-Trichloropyrimidine(cas: 3764-01-0) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Quality Control of 2,4,6-Trichloropyrimidine
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia