On May 31, 2011, Wenglowsky, Steve; Ren, Li; Ahrendt, Kateri A.; Laird, Ellen R.; Aliagas, Ignacio; Alicke, Bruno; Buckmelter, Alex J.; Choo, Edna F.; Dinkel, Victoria; Feng, Bainian; Gloor, Susan L.; Gould, Stephen E.; Gross, Stefan; Gunzner-Toste, Janet; Hansen, Joshua D.; Hatzivassiliou, Georgia; Liu, Bonnie; Malesky, Kim; Mathieu, Simon; Newhouse, Brad; Raddatz, Nicholas J.; Ran, Yingqing; Rana, Sumeet; Randolph, Nikole; Risom, Tyler; Rudolph, Joachim; Savage, Scott; Selby, LeAnn T.; Shrag, Michael; Song, Kyung; Sturgis, Hillary L.; Voegtli, Walter C.; Wen, Zhaoyang; Willis, Brandon S.; Woessner, Richard D.; Wu, Wen-I.; Young, Wendy B.; Grina, Jonas published an article.Computed Properties of 1186608-73-0 The title of the article was Pyrazolopyridine Inhibitors of B-RafV600E. Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors. And the article contained the following:
The V600E mutation of B-Raf kinase results in constitutive activation of the MAPK signaling pathway and is present in approx. 7% of all cancers. Using structure-based design, a novel series of pyrazolopyridine inhibitors of B-RafV600E was developed. Optimization led to the identification of 3-methoxy pyrazolopyridines 17 and 19, potent, selective, and orally bioavailable agents that inhibited tumor growth in a mouse xenograft model driven by B-RafV600E with no effect on body weight On the basis of their in vivo efficacy and preliminary safety profiles, 17 and 19 were selected for further preclin. evaluation. The experimental process involved the reaction of 3-Methyl-1H-pyrazolo[3,4-b]pyridin-5-amine(cas: 1186608-73-0).Computed Properties of 1186608-73-0
The Article related to pyrazolopyridine derivative braf kinase inhibitor preparation antitumor pharmacokinetics toxicity, b-rafv600e, mapk pathway, amorphous spray-dried dispersion, pyrazolopyridine, targeted therapy and other aspects.Computed Properties of 1186608-73-0
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics