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414864-00-9,MFCD08064035
Catalog No.:AA00BZP6

414864-00-9 | Belinostat

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10mg
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1g
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  • Technical Information
  • Properties
  • Literature
Technical Information
Catalog Number:
AA00BZP6
Chemical Name:
Belinostat
CAS Number:
414864-00-9
Molecular Formula:
C15H14N2O4S
Molecular Weight:
318.3477
MDL Number:
MFCD08064035
SMILES:
ONC(=O)C=Cc1cccc(c1)S(=O)(=O)Nc1ccccc1
NSC Number:
726630
Properties
Computed Properties
 
Complexity:
492  
Covalently-Bonded Unit Count:
1  
Defined Bond Stereocenter Count:
1  
Heavy Atom Count:
22  
Hydrogen Bond Acceptor Count:
5  
Hydrogen Bond Donor Count:
3  
Rotatable Bond Count:
5  
XLogP3:
1.7  

Literature

Title: Investigation of belinostat-induced genomic instability by molecular cytogenetic analysis and pathway-focused gene expression profiling.

Journal: Toxicology and applied pharmacology 20180701

Title: Inhibition of histone H3K27 demethylases selectively modulates inflammatory phenotypes of natural killer cells.

Journal: The Journal of biological chemistry 20180216

Title: Targeting histone deacetylases in T-cell lymphoma.

Journal: Leukemia & lymphoma 20170601

Title: Fingerprinting of neurotoxic compounds using a mouse embryonic stem cell dual luminescence reporter assay.

Journal: Archives of toxicology 20170101

Title: Definition of transcriptome-based indices for quantitative characterization of chemically disturbed stem cell development: introduction of the STOP-Tox(ukn) and STOP-Tox(ukk) tests.

Journal: Archives of toxicology 20170101

Title: Belinostat for Relapsed or Refractory Peripheral T-Cell Lymphoma.

Journal: Journal of the advanced practitioner in oncology 20160301

Title: Belinostat, a potent HDACi, exerts antileukaemic effect in human acute promyelocytic leukaemia cells via chromatin remodelling.

Journal: Journal of cellular and molecular medicine 20150701

Title: A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors.

Journal: Archives of toxicology 20150101

Title: Epigenetic and molecular mechanisms underlying the antileukemic activity of the histone deacetylase inhibitor belinostat in human acute promyelocytic leukemia cells.

Journal: Anti-cancer drugs 20140901

Title: Glucuronidation by UGT1A1 is the dominant pathway of the metabolic disposition of belinostat in liver cancer patients.

Journal: PloS one 20130101

Title: Histone acetylation-mediated regulation of the Hippo pathway.

Journal: PloS one 20130101

Title: Epigenetic therapy using belinostat for patients with unresectable hepatocellular carcinoma: a multicenter phase I/II study with biomarker and pharmacokinetic analysis of tumors from patients in the Mayo Phase II Consortium and the Cancer Therapeutics Research Group.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20120920

Title: HDAC inhibitors synergize antiproliferative effect of sorafenib in renal cell carcinoma cells.

Journal: Anticancer research 20120801

Title: Phase II activity of belinostat (PXD-101), carboplatin, and paclitaxel in women with previously treated ovarian cancer.

Journal: International journal of gynecological cancer : official journal of the International Gynecological Cancer Society 20120701

Title: A phase II evaluation of belinostat and carboplatin in the treatment of recurrent or persistent platinum-resistant ovarian, fallopian tube, or primary peritoneal carcinoma: a Gynecologic Oncology Group study.

Journal: Gynecologic oncology 20120501

Title: Differential effects of PXD101 (belinostat) on androgen-dependent and androgen-independent prostate cancer models.

Journal: International journal of oncology 20120301

Title: Histone deacetylase inhibition increases levels of choline kinase α and phosphocholine facilitating noninvasive imaging in human cancers.

Journal: Cancer research 20120215

Title: Phase II study of the histone deacetylase inhibitor belinostat (PXD101) for the treatment of myelodysplastic syndrome (MDS).

Journal: Annals of hematology 20120101

Title: Experimental in vivo and in vitro treatment with a new histone deacetylase inhibitor belinostat inhibits the growth of pancreatic cancer.

Journal: BMC cancer 20120101

Title: Belinostat: clinical applications in solid tumors and lymphoma.

Journal: Expert opinion on investigational drugs 20111201

Title: Schedule-dependent synergy of histone deacetylase inhibitors with DNA damaging agents in small cell lung cancer.

Journal: Cell cycle (Georgetown, Tex.) 20110915

Title: Histone deacetylase inhibitor belinostat represses survivin expression through reactivation of transforming growth factor beta (TGFbeta) receptor II leading to cancer cell death.

Journal: The Journal of biological chemistry 20110902

Title: The histone deacetylase inhibitor PXD101 increases the efficacy of irinotecan in in vitro and in vivo colon cancer models.

Journal: Cancer chemotherapy and pharmacology 20110801

Title: Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.

Journal: Journal of medicinal chemistry 20110714

Title: Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors.

Journal: Journal of medicinal chemistry 20110714

Title: Assessment of objective responses using volumetric evaluation in advanced thymic malignancies and metastatic non-small cell lung cancer.

Journal: Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20110701

Title: Pharmacokinetic and pharmacodynamic properties of an oral formulation of the histone deacetylase inhibitor Belinostat (PXD101).

Journal: Cancer chemotherapy and pharmacology 20110601

Title: Phase II study of belinostat in patients with recurrent or refractory advanced thymic epithelial tumors.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20110520

Title: Discovery, synthesis, and pharmacological evaluation of spiropiperidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors.

Journal: Journal of medicinal chemistry 20110428

Title: Bortezomib interacts synergistically with belinostat in human acute myeloid leukaemia and acute lymphoblastic leukaemia cells in association with perturbations in NF-κB and Bim.

Journal: British journal of haematology 20110401

Title: Synergistic activity of histone deacetylase and proteasome inhibition against pancreatic and hepatocellular cancer cell lines.

Journal: Anticancer research 20110401

Title: Histone deacetylase inhibitors for purging HIV-1 from the latent reservoir.

Journal: Molecular medicine (Cambridge, Mass.) 20110101

Title: Liposomes loaded with histone deacetylase inhibitors for breast cancer therapy.

Journal: International journal of pharmaceutics 20100915

Title: A sensitive and specific liquid chromatography-tandem mass spectrometric method for determination of belinostat in plasma from liver cancer patients.

Journal: Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20100915

Title: Proteomic profiling of human colon cancer cells treated with the histone deacetylase inhibitor belinostat.

Journal: Electrophoresis 20100801

Title: A phase I study of the safety and pharmacokinetics of the histone deacetylase inhibitor belinostat administered in combination with carboplatin and/or paclitaxel in patients with solid tumours.

Journal: British journal of cancer 20100629

Title: Phase II trial of the histone deacetylase inhibitor belinostat in women with platinum resistant epithelial ovarian cancer and micropapillary (LMP) ovarian tumours.

Journal: European journal of cancer (Oxford, England : 1990) 20100601

Title: Chemical phylogenetics of histone deacetylases.

Journal: Nature chemical biology 20100301

Title: Troglitazone inhibits histone deacetylase activity in breast cancer cells.

Journal: Cancer letters 20100227

Title: Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors.

Journal: Journal of medicinal chemistry 20100128

Title: Romidepsin and belinostat synergize the antineoplastic effect of bortezomib in mantle cell lymphoma.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20100115

Title: A novel histone deacetylase inhibitor, CG0006, induces cell death through both extrinsic and intrinsic apoptotic pathways.

Journal: Anti-cancer drugs 20091001

Title: Gene expression-signature of belinostat in cell lines is specific for histone deacetylase inhibitor treatment, with a corresponding signature in xenografts.

Journal: Anti-cancer drugs 20090901

Title: Clinical studies of histone deacetylase inhibitors.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20090615

Title: Belinostat: a new broad acting antineoplastic histone deacetylase inhibitor.

Journal: Expert opinion on investigational drugs 20090401

Title: Combined inhibition of DNA methylation and histone acetylation enhances gene re-expression and drug sensitivity in vivo.

Journal: British journal of cancer 20090310

Title: Inhibition of HDAC6-dependent carcinogenesis: emerging, new therapeutic options besides belinostat.

Journal: International journal of cancer 20090115

Title: Phase II study of belinostat (PXD101), a histone deacetylase inhibitor, for second line therapy of advanced malignant pleural mesothelioma.

Journal: Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20090101

Title: Integrative analysis of epigenetic modulation in melanoma cell response to decitabine: clinical implications.

Journal: PloS one 20090101

Title: Histone deacetylase inhibitors: apoptotic effects and clinical implications (Review).

Journal: International journal of oncology 20081001

Title: A phase I clinical trial of the histone deacetylase inhibitor belinostat in patients with advanced hematological neoplasia.

Journal: European journal of haematology 20080901

Title: Plasma and cerebrospinal fluid pharmacokinetics of the histone deacetylase inhibitor, belinostat (PXD101), in non-human primates.

Journal: Cancer chemotherapy and pharmacology 20080801

Title: Monitoring the effect of belinostat in solid tumors by H4 acetylation.

Journal: APMIS : acta pathologica, microbiologica, et immunologica Scandinavica 20080501

Title: Activity of the histone deacetylase inhibitor belinostat (PXD101) in preclinical models of prostate cancer.

Journal: International journal of cancer 20080315

Title: Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.

Journal: Bioorganic & medicinal chemistry letters 20080315

Title: A phase 1 pharmacokinetic and pharmacodynamic study of the histone deacetylase inhibitor belinostat in patients with advanced solid tumors.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20080201

Title: Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors.

Journal: The Biochemical journal 20080115

Title: Interactions between bortezomib and romidepsin and belinostat in chronic lymphocytic leukemia cells.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20080115

Title: Identification of predictive biomarkers for the histone deacetylase inhibitor belinostat in a panel of human cancer cell lines.

Journal: Cancer biomarkers : section A of Disease markers 20080101

Title: Differential effects of class I isoform histone deacetylase depletion and enzymatic inhibition by belinostat or valproic acid in HeLa cells.

Journal: Molecular cancer 20080101

Title: Functional characteristics and gene expression profiles of primary acute myeloid leukaemia cells identify patient subgroups that differ in susceptibility to histone deacetylase inhibitors.

Journal: International journal of oncology 20071201

Title: The histone deacetylase inhibitor, PXD101, potentiates bortezomib-induced anti-multiple myeloma effect by induction of oxidative stress and DNA damage.

Journal: British journal of haematology 20071101

Title: The histone deacetylase inhibitor PXD101 synergises with 5-fluorouracil to inhibit colon cancer cell growth in vitro and in vivo.

Journal: Cancer chemotherapy and pharmacology 20070701

Title: A simple and sensitive high-performance liquid chromatographic method for quantification of PXD101, a histone deacetylase inhibitor in human plasma.

Journal: Therapeutic drug monitoring 20070401

Title: HDAC inhibitors and cardiac safety.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20070201

Title: Nuclear factor-kappaB p65 small interfering RNA or proteasome inhibitor bortezomib sensitizes head and neck squamous cell carcinomas to classic histone deacetylase inhibitors and novel histone deacetylase inhibitor PXD101.

Journal: Molecular cancer therapeutics 20070101

Title: The histone deacetylase inhibitor belinostat (PXD101) suppresses bladder cancer cell growth in vitro and in vivo.

Journal: Journal of translational medicine 20070101

Title: Activity of PXD101, a histone deacetylase inhibitor, in preclinical ovarian cancer studies.

Journal: Molecular cancer therapeutics 20060801

Title: Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histone deacetylase inhibitor PXD101.

Journal: Molecular cancer therapeutics 20030801

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