In 2018,Journal of Medicinal Chemistry included an article by Rageot, Denise; Bohnacker, Thomas; Melone, Anna; Langlois, Jean-Baptiste; Borsari, Chiara; Hillmann, Petra; Sele, Alexander M.; Beaufils, Florent; Zvelebil, Marketa; Hebeisen, Paul; Loscher, Wolfgang; Burke, John; Fabbro, Doriano; Wymann, Matthias P.. Name: 2,4,6-Trichloropyrimidine. The article was titled 《Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders》. The information in the text is summarized as follows:
Mechanistic target of rapamycin (mTOR) promotes cell proliferation, growth, and survival and is overactivated in many tumors and central nervous system disorders. I is a novel, potent, selective, and brain penetrable inhibitor of mTORC1/2 kinase. I showed excellent selectivity for mTOR over PI3K and protein kinases and efficiently prevented cancer cell growth in a 66 cancer cell line panel. In C57BL/6J and Sprague-Dawley mice, maximum concentration (Cmax) in plasma and brain was reached after 30 min, with a half-life (t1/2) > 5 h. In an ovarian carcinoma mouse xenograft model (OVCAR-3), daily dosing of I inhibited tumor growth significantly. Moreover, I attenuated epileptic seizures in a tuberous sclerosis complex (TSC) mouse model. In conclusion, I inhibits mTOR kinase potently and selectively, shows antitumor effects in vitro and in vivo, and promises advantages in CNS indications due to its brain/plasma distribution ratio. The experimental part of the paper was very detailed, including the reaction process of 2,4,6-Trichloropyrimidine(cas: 3764-01-0Name: 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.Name: 2,4,6-Trichloropyrimidine
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia