Potent and selective pan-aurora kinase inhibitor that binds aurora kinase in the DFG-in conformation and exhibits anticancer efficacy in vitro and in vivo.
SNS-314 is a potent pan-aurora kinases inhibitor (IC50 = 9/31/3 nM against aurora kinase A/B/C or aurora 2/1/3) that binds aurora kinase in the DFG-in conformation and exhibits great selectivity against a panel of 219 kinases (>5-, >12-, >14-, >15-, >82-, >84-fold selectivity for aurora A over TrkB, TrkA, Flt4, Fms, DDR2, Axl, respectively; >100-fold selectivity over c-Raf and the remaining kinases). SNS-314 downregulates cellular histone H3 Ser10 (HH3 Ser10) phosphorylation (IC50 <16 nM) and exhibits potent antiproliferation activity in HCT116 human colon cancer cultures in vitro (IC50 = 5 nM). When applied in vivo, HCT116 likewise reduces pHH3 (Ser10) level in tumor tissue (by 75-100% 6 hrs post 50 mg/kg i.p. dosage) and suppresses tumor growth (100 mg/kg/day, 5 days on, 9 days off; 150 mg/kg biweekly x3), as well as potentiates docetaxel antitumor efficacy in a mouse HCT116 xenograft model in vivo (42.5 mg SNS-314/kg followed by 10 mg docetaxel/kg 24 hr later; biweekly x3).
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11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 3
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Not applicable
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Cancer chemotherapy and pharmacology, 65(4), 707-717 (2009-08-04)
The Aurora family of serine/threonine kinases (Aurora-A, Aurora-B, and Aurora-C) plays a key role in cells orderly progression through mitosis. Elevated expression levels of Aurora kinases have been detected in a high percentage of melanoma, colon, breast, ovarian, gastric, and
Journal of cellular physiology, 231(8), 1784-1795 (2015-12-15)
The aim of this paper is based on the use of a hyaluronic acid hydrogel of Quercetin tested alone and in combination to an inhibitor of Aurora Kinase type A and B (SNS-314) on human medullary and papillary thyroid cancer
Investigational new drugs, 34(5), 531-540 (2016-05-15)
New therapeutic targets are needed to fight cancer. Aurora kinases (AK) were recently identified as vital key regulators of cell mitosis and have consequently been investigated as therapeutic targets in preclinical and clinical studies. Aurora kinase inhibitors (AKI) have been
This communication describes the discovery of a novel series of Aurora kinase inhibitors. Key SAR and critical binding elements are discussed. Some of the more advanced analogues potently inhibit cellular proliferation and induce phenotypes consistent with Aurora kinase inhibition. In
The intersection of small molecular weight drugs and antibody-based therapeutics is rarely studied in large scale. Both types of agents are currently part of the cancer armamentarium. However, very little is known about how to combine them in optimal ways.
Notre équipe de scientifiques dispose d'une expérience dans tous les secteurs de la recherche, notamment en sciences de la vie, science des matériaux, synthèse chimique, chromatographie, analyse et dans de nombreux autres domaines..
