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Ref Type Journal Article
PMID (24900437)
Authors Haddach M, Michaux J, Schwaebe MK, Pierre F, O'Brien SE, Borsan C, Tran J, Raffaele N, Ravula S, Drygin D, Siddiqui-Jain A, Darjania L, Stansfield R, Proffitt C, Macalino D, Streiner N, Bliesath J, Omori M, Whitten JP, Anderes K, Rice WG, Ryckman DM
Title Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor.
Journal ACS medicinal chemistry letters
Vol 3
Issue 2
Date 2012 Feb 9
URL
Abstract Text 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.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
CX-6258 CX-6258 2 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
CX-6258 PIM Inhibitor (Pan) 9 CX-6258 is an inhibitor of PIM1, PIM2, PIM3 and Histone H3-associated protein serine/threonine kinase (HASPIN), which may potentially result in antitumor activity (PMID: 24900437) and may overcome tumor resistance to RAF/MEK-inhibitors (PMID: 31882401).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
Unknown unknown prostate cancer not applicable CX-6258 Preclinical - Cell line xenograft Actionable In a preclinical study, CX-6258 inhibited tumor growth in human prostate cancer cell line xenograft models (PMID: 24900437). 24900437
Unknown unknown acute myeloid leukemia not applicable CX-6258 Preclinical - Cell line xenograft Actionable In a preclinical study, CX-6528 inhibited tumor growth in human acute myeloid leukemia cell line xenograft models (PMID: 24900437). 24900437