title: Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor.
abstract: 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.
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: Mustapha
authors.initials: M
authors.lastname: Haddach
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: Jerome
authors.initials: J
authors.lastname: Michaux
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: Michael K
authors.initials: MK
authors.lastname: Schwaebe
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: Fabrice
authors.initials: F
authors.lastname: Pierre
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: Sean E
authors.initials: SE
authors.lastname: O'Brien
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: Cosmin
authors.initials: C
authors.lastname: Borsan
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: Joe
authors.initials: J
authors.lastname: Tran
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: Nicholas
authors.initials: N
authors.lastname: Raffaele
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: Suchitra
authors.initials: S
authors.lastname: Ravula
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: Denis
authors.initials: D
authors.lastname: Drygin
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: Adam
authors.initials: A
authors.lastname: Siddiqui-Jain
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: Levan
authors.initials: L
authors.lastname: Darjania
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: Ryan
authors.initials: R
authors.lastname: Stansfield
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: Chris
authors.initials: C
authors.lastname: Proffitt
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: Diwata
authors.initials: D
authors.lastname: Macalino
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: Nicole
authors.initials: N
authors.lastname: Streiner
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: Joshua
authors.initials: J
authors.lastname: Bliesath
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: May
authors.initials: M
authors.lastname: Omori
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: Jeffrey P
authors.initials: JP
authors.lastname: Whitten
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: Kenna
authors.initials: K
authors.lastname: Anderes
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: William G
authors.initials: WG
authors.lastname: Rice
authors.affiliation: Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
authors.forename: David M
authors.initials: DM
authors.lastname: Ryckman
keywords: CX-6258; MV-4-11; PC3; Pim-1; Pim-2; Pim-3