1007206-24-7

Upstream product

• 462-08-8 pyridin-3-ylamine 
• 1007206-27-0 4-[4,6-dichloro-5-(2-chloroethyl)-pyrimidin-2-yl]-morpholine 

Downstream Products

• 1272403-08-3 C₃₅H₃₆N₈O₃ 
• 1007206-86-1 3-(2-morpholin-4-yl-7-pyridin-3-yl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)-benzenesulfonamide 
• 1007213-69-5 3-(2-morpholin-4-yl-7-pyridin-3-yl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)-benzoic acid methyl ester 

Relevant academic research and scientific papers

Discovery and biological activity of a novel class i PI3K inhibitor, CH5132799

Phosphatidylinositol 3-kinase (PI3K) is a lipid kinase and a promising therapeutic target for cancer. Using structure-based drug design (SBDD), we have identified novel PI3K inhibitors with a dihydropyrrolopyrimidine skeleton. Metabolic stability of the first lead series was drastically improved by replacing phenol with aminopyrimidine moiety. CH5132799, a novel class I PI3K inhibitor, exhibited a strong inhibitory activity especially against PI3Kα (IC50 = 0.014 μM). In human tumor cell lines with PI3K pathway activation, CH5132799 showed potent antiproliferative activity. CH5132799 is orally available and showed significant antitumor activity in PI3K pathway-activated human cancer xenograft models in mice.

BICYCLIC HETEROARENES AND METHODS OF THEIR USE

Disclosed are compounds useful in the treatment of neurological disorders. The compounds described herein, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological diseases.