658084-64-1 | Fk866

658084-64-1   

N-((S)-1-(((S)-1-((4-(bromomethyl)phenyl)amino)-1-oxopropan2-yl)amino)-3-methyl-1-oxobutan-2-yl)-6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanamide 

  76-05-1   

3-((E)-3-((4-(1-benzoylpiperidin-4-yl)butyl)amino)-3-oxoprop-1-en-1-yl)-1-(4-((S)-2-((S)-2-(6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanamido)-3-methylbutanamido)propanamido)benzyl)pyridin-1-ium2,2,2-trifluoroacetate 

[1]CurrentPatentAssignee:SEAGENINC-WO2018/201087,2018,A1Locationinpatent:Paragraph0889;0910;0911

658084-64-1   

(2S,3R,4S,5S,6S)-2-(2-(3-(((9H-fluoren-9-yl)methoxy)carbonyl)amino)propanamido)-4-((bromomethyl)phenoxy)-6-(methoxycarbonyl)tetrahydro-2H-pyran-3,4,5-triyltriacetate 

  76-05-1   

1-(3-(3-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)propanamido)-4-(((2S,3R,4S,5S,6S)-3,4,5-triacetoxy-6-(methoxycarbonyl)tetrahydro-2H-pyran-2-yl)oxy)benzyl)-3-((E)-3-((4-(1-benzoylpiperidin-4-yl)butyl)amino)-3-oxoprop-1-en-1-yl)pyridin-1-ium2,2,2-trifluoroacetate 

[1]CurrentPatentAssignee:SEAGENINC-WO2018/201087,2018,A1Locationinpatent:Paragraph0889;0895;0896;0897

658084-64-1   

1-(3-(3-aminopropanamido)-4-(((2S,3R,4S,5S,6S)-6-carboxy-3,4,5-trihydroxytetrahydro-2H-pyran-2-yl)oxy)benzyl)-3-((E)-3-((4-(1-benzoylpiperidin-4-yl)butyl)amino)-3-oxoprop-1-en-1-yl)pyridin-1-ium2,2,2-trifluoroacetate 

[1]CurrentPatentAssignee:SEAGENINC-WO2018/201087,2018,A1

658084-64-1   

3-((E)-3-((4-(1-benzoylpiperidin-4-yl)butyl)amino)-3-oxoprop-1-en-1-yl)-1-(4-(((2S,3R,4S,5S,6S)-6-carboxy-3,4,5-trihydroxytetrahydro-2H-pyran-2-yl)oxy)-3-(3-(6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanamido)propanamido)benzyl)pyridin-1-ium2,2,2-trifluoroacetate 

[1]CurrentPatentAssignee:SEAGENINC-WO2018/201087,2018,A1

658084-64-1   

3-((E)-3-((4-(1-benzoylpiperidin-4-yl)butyl)amino)-3-oxoprop-1-en-1-yl)-1-(3-(3-((S)-3-((tert-butoxycarbonyl)amino)-2-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)propanamido)propanamido)-4-(((2S,3R,4S,5S,6S)-6-carboxy-3,4,5-trihydroxytetrahydro-2H-pyran-2-yl)oxy)benzyl)pyridin-1-ium2,2,2-trifluoroacetate 

[1]CurrentPatentAssignee:SEAGENINC-WO2018/201087,2018,A1

Title: Inhibition of nicotinamide phosphoribosyltransferase and depletion of nicotinamide adenine dinucleotide contribute to arsenic trioxide suppression of oral squamous cell carcinoma.

Journal: Toxicology and applied pharmacology 20170915

Title: Retinal toxicity, in vivo and in vitro, associated with inhibition of nicotinamide phosphoribosyltransferase.

Journal: Toxicological sciences : an official journal of the Society of Toxicology 20150301

Title: On-target effect of FK866, a nicotinamide phosphoribosyl transferase inhibitor, by apoptosis-mediated death in chronic lymphocytic leukemia cells.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20140915

Title: Elevated microRNA-34a in obesity reduces NAD+ levels and SIRT1 activity by directly targeting NAMPT.

Journal: Aging cell 20131201

Title: Visfatin is expressed in human granulosa cells: regulation by metformin through AMPK/SIRT1 pathways and its role in steroidogenesis.

Journal: Molecular human reproduction 20130501

Title: Nicotinamide phosphoribosyl transferase (Nampt) is a target of microRNA-26b in colorectal cancer cells.

Journal: PloS one 20130101

Title: Synthetic lethality of PARP and NAMPT inhibition in triple-negative breast cancer cells.

Journal: EMBO molecular medicine 20121001

Title: Inhibition of NAMPT pathway by FK866 activates the function of p53 in HEK293T cells.

Journal: Biochemical and biophysical research communications 20120803

Title: Role of deleted in breast cancer 1 (DBC1) protein in SIRT1 deacetylase activation induced by protein kinase A and AMP-activated protein kinase.

Journal: The Journal of biological chemistry 20120706

Title: NAD+ levels control Ca2+ store replenishment and mitogen-induced increase of cytosolic Ca2+ by Cyclic ADP-ribose-dependent TRPM2 channel gating in human T lymphocytes.

Journal: The Journal of biological chemistry 20120615

Title: Inhibition of nicotinamide phosphoribosyltransferase modifies LPS-induced inflammatory responses of human monocytes.

Journal: Innate immunity 20120601

Title: Proinflammatory actions of visfatin/nicotinamide phosphoribosyltransferase (Nampt) involve regulation of insulin signaling pathway and Nampt enzymatic activity.

Journal: The Journal of biological chemistry 20120427

Title: NAMPT pathway is involved in the FOXO3a-mediated regulation of GADD45A expression.

Journal: Biochemical and biophysical research communications 20120420

Title: The role of sirtuin 2 activation by nicotinamide phosphoribosyltransferase in the aberrant proliferation and survival of myeloid leukemia cells.

Journal: Haematologica 20120401

Title: Anti-proliferation effect of APO866 on C6 glioblastoma cells by inhibiting nicotinamide phosphoribosyltransferase.

Journal: European journal of pharmacology 20120115

Title: Pre-B-cell colony-enhancing factor exerts a neuronal protection through its enzymatic activity and the reduction of mitochondrial dysfunction in in vitro ischemic models.

Journal: Journal of neurochemistry 20120101

Title: Nicotinamide phosphoribosyltransferase: a potent therapeutic target in non-small cell lung cancer with epidermal growth factor receptor-gene mutation.

Journal: Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20120101

Title: The NAMPT inhibitor FK866 reverts the damage in spinal cord injury.

Journal: Journal of neuroinflammation 20120101

Title: Overexpression of Nampt in gastric cancer and chemopotentiating effects of the Nampt inhibitor FK866 in combination with fluorouracil.

Journal: Oncology reports 20111101

Title: Reciprocal potentiation of the antitumoral activities of FK866, an inhibitor of nicotinamide phosphoribosyltransferase, and etoposide or cisplatin in neuroblastoma cells.

Journal: The Journal of pharmacology and experimental therapeutics 20110901

Title: Suppression of leukocyte infiltration and cartilage degradation by selective inhibition of pre-B cell colony-enhancing factor/visfatin/nicotinamide phosphoribosyltransferase: Apo866-mediated therapy in human fibroblasts and murine collagen-induced arthritis.

Journal: Arthritis and rheumatism 20110701

Title: Design, synthesis and X-ray crystallographic study of NAmPRTase inhibitors as anti-cancer agents.

Journal: European journal of medicinal chemistry 20110401

Title: Overcoming temozolomide resistance in glioblastoma via dual inhibition of NAD+ biosynthesis and base excision repair.

Journal: Cancer research 20110315

Title: Synergistic interactions between HDAC and sirtuin inhibitors in human leukemia cells.

Journal: PloS one 20110101

Title: Potent synergistic interaction between the Nampt inhibitor APO866 and the apoptosis activator TRAIL in human leukemia cells.

Journal: Experimental hematology 20101101

Title: Inhibition of nicotinamide phosphoribosyltransferase: cellular bioenergetics reveals a mitochondrial insensitive NAD pool.

Journal: The Journal of biological chemistry 20101029

Title: Nampt/PBEF/visfatin and cancer.

Journal: Cancer biology & therapy 20100715

Title: A combination of the metabolic enzyme inhibitor APO866 and the immune adjuvant L-1-methyl tryptophan induces additive antitumor activity.

Journal: Experimental biology and medicine (Maywood, N.J.) 20100701

Title: A preclinical study on the rescue of normal tissue by nicotinic acid in high-dose treatment with APO866, a specific nicotinamide phosphoribosyltransferase inhibitor.

Journal: Molecular cancer therapeutics 20100601

Title: Safety and efficacy of NAD depleting cancer drugs: results of a phase I clinical trial of CHS 828 and overview of published data.

Journal: Cancer chemotherapy and pharmacology 20100501

Title: Inhibition of lactate dehydrogenase A induces oxidative stress and inhibits tumor progression.

Journal: Proceedings of the National Academy of Sciences of the United States of America 20100202

Title: Target enzyme mutations are the molecular basis for resistance towards pharmacological inhibition of nicotinamide phosphoribosyltransferase.

Journal: BMC cancer 20100101

Title: Crystal structure of Rattus norvegicus Visfatin/PBEF/Nampt in complex with an FK866-based inhibitor.

Journal: Molecules and cells 20090630

Title: APO866 activity in hematologic malignancies: a preclinical in vitro study.

Journal: Blood 20090604

Title: Detection and pharmacological modulation of nicotinamide mononucleotide (NMN) in vitro and in vivo.

Journal: Biochemical pharmacology 20090515

Title: Circadian control of the NAD+ salvage pathway by CLOCK-SIRT1.

Journal: Science (New York, N.Y.) 20090501

Title: Circadian clock feedback cycle through NAMPT-mediated NAD+ biosynthesis.

Journal: Science (New York, N.Y.) 20090501

Title: Circadian rhythms. A circadian loop asSIRTs itself.

Journal: Science (New York, N.Y.) 20090501

Title: The NAD biosynthesis inhibitor APO866 has potent antitumor activity against hematologic malignancies.

Journal: Blood 20090402

Title: Catastrophic NAD+ depletion in activated T lymphocytes through Nampt inhibition reduces demyelination and disability in EAE.

Journal: PloS one 20090101

Title: Extracellular Nampt promotes macrophage survival via a nonenzymatic interleukin-6/STAT3 signaling mechanism.

Journal: The Journal of biological chemistry 20081212

Title: Visfatin: a new player in mesangial cell physiology and diabetic nephropathy.

Journal: American journal of physiology. Renal physiology 20081101

Title: Weak coupling of ATP hydrolysis to the chemical equilibrium of human nicotinamide phosphoribosyltransferase.

Journal: Biochemistry 20081021

Title: Synthesis and biological evaluation of isosteric analogues of FK866, an inhibitor of NAD salvage.

Journal: ChemMedChem 20080501

Title: NAD depletion by FK866 induces autophagy.

Journal: Autophagy 20080401

Title: Anticancer agent CHS-828 inhibits cellular synthesis of NAD.

Journal: Biochemical and biophysical research communications 20080321

Title: Characterization of NAD uptake in mammalian cells.

Journal: The Journal of biological chemistry 20080307

Title: The pharmacokinetics, toxicities, and biologic effects of FK866, a nicotinamide adenine dinucleotide biosynthesis inhibitor.

Journal: Investigational new drugs 20080201

Title: Nicotinamide adenine dinucleotide metabolism as an attractive target for drug discovery.

Journal: Expert opinion on therapeutic targets 20070501

Title: Crystal structure of visfatin/pre-B cell colony-enhancing factor 1/nicotinamide phosphoribosyltransferase, free and in complex with the anti-cancer agent FK-866.

Journal: Journal of molecular biology 20060908

Title: Chemopotentiating effects of a novel NAD biosynthesis inhibitor, FK866, in combination with antineoplastic agents.

Journal: European journal of medical research 20060830

Title: Molecular basis for the inhibition of human NMPRTase, a novel target for anticancer agents.

Journal: Nature structural & molecular biology 20060701

Title: Metabolic signatures associated with a NAD synthesis inhibitor-induced tumor apoptosis identified by 1H-decoupled-31P magnetic resonance spectroscopy.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20050501

Title: FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis.

Journal: Cancer research 20031101

Title: Antiangiogenic potency of FK866/K22.175, a new inhibitor of intracellular NAD biosynthesis, in murine renal cell carcinoma.

Journal: Anticancer research 20030101

Title: Cea M, et al. Targeting NAD+ salvage pathway induces autophagy in multiple myeloma cells via mTORC1 and extracellular signal-regulated kinase (ERK1/2) inhibition. Blood. 2012 Oct 25;120(17):3519-29.

Title: Magnone M, et al. NAD+ levels control Ca2+ store replenishment and mitogen-induced increase of cytosolic Ca2+ by Cyclic ADP-ribose-dependent TRPM2 channel gating in human T lymphocytes. J Biol Chem. 2012 Jun 15;287(25):21067-81.

Title: Thakur BK, et al. Inhibition of NAMPT pathway by FK866 activates the function of p53 in HEK293T cells. Biochem Biophys Res Commun. 2012 Aug 3;424(3):371-7.