1353859-00-3Relevant articles and documents
Discovery of CX-6258. A potent, selective, and orally efficacious pan-pim kinases inhibitor
Haddach, Mustapha,Michaux, Jerome,Schwaebe, Michael K.,Pierre, Fabrice,O'Brien, Sean E.,Borsan, Cosmin,Tran, Joe,Raffaele, Nicholas,Ravula, Suchitra,Drygin, Denis,Siddiqui-Jain, Adam,Darjania, Levan,Stansfield, Ryan,Proffitt, Chris,MacAlino, Diwata,Streiner, Nicole,Bliesath, Joshua,Omori, May,Whitten, Jeffrey P.,Anderes, Kenna,Rice, William G.,Ryckman, David M.
supporting information; experimental part, p. 135 - 139 (2012/04/04)
Structure-activity relationship analysis in a series of 3-(5-((2-oxoindolin-3-ylidene)methyl)furan-2-yl)amides identified compound 13, a pan-Pim kinases inhibitor with excellent biochemical potency and kinase selectivity. Compound 13 exhibited in vitro synergy with chemotherapeutics and robust in vivo efficacy in two Pim kinases driven tumor models.