414864-00-9 | Belinostat

Packsize	Purity	Availability	Price	Discounted Price
10mg	≥98%	in stock	$44.00	$31.00
1g	97%	in stock	$124.00	$87.00

Description

• Catalog Number: AF59382
• 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

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

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

  Toxicology and applied pharmacology 20180701

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

  The Journal of biological chemistry 20180216

• Targeting histone deacetylases in T-cell lymphoma.

  Leukemia & lymphoma 20170601

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

  Archives of toxicology 20170101

• 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.

  Archives of toxicology 20170101

• Belinostat for Relapsed or Refractory Peripheral T-Cell Lymphoma.

  Journal of the advanced practitioner in oncology 20160301

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

  Journal of cellular and molecular medicine 20150701

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

  Archives of toxicology 20150101

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

  Anti-cancer drugs 20140901

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

  PloS one 20130101

• Histone acetylation-mediated regulation of the Hippo pathway.

  PloS one 20130101

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

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

  Anticancer research 20120801

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

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

• 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.

  Gynecologic oncology 20120501

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

  International journal of oncology 20120301

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

  Cancer research 20120215

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

  Annals of hematology 20120101

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

  BMC cancer 20120101

• Belinostat: clinical applications in solid tumors and lymphoma.

  Expert opinion on investigational drugs 20111201

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

  Cell cycle (Georgetown, Tex.) 20110915

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

  The Journal of biological chemistry 20110902

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

  Cancer chemotherapy and pharmacology 20110801

• 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 of medicinal chemistry 20110714

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

  Journal of medicinal chemistry 20110714

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

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

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

  Cancer chemotherapy and pharmacology 20110601

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

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

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

  Journal of medicinal chemistry 20110428

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

  British journal of haematology 20110401

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

  Anticancer research 20110401

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

  Molecular medicine (Cambridge, Mass.) 20110101

• Liposomes loaded with histone deacetylase inhibitors for breast cancer therapy.

  International journal of pharmaceutics 20100915

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

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

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

  Electrophoresis 20100801

• 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.

  British journal of cancer 20100629

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

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

• Chemical phylogenetics of histone deacetylases.

  Nature chemical biology 20100301

• Troglitazone inhibits histone deacetylase activity in breast cancer cells.

  Cancer letters 20100227

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

  Journal of medicinal chemistry 20100128

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

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

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

  Anti-cancer drugs 20091001

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

  Anti-cancer drugs 20090901

• Clinical studies of histone deacetylase inhibitors.

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

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

  Expert opinion on investigational drugs 20090401

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

  British journal of cancer 20090310

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

  International journal of cancer 20090115

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

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

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

  PloS one 20090101

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

  International journal of oncology 20081001

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

  European journal of haematology 20080901

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

  Cancer chemotherapy and pharmacology 20080801

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

  APMIS : acta pathologica, microbiologica, et immunologica Scandinavica 20080501

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

  International journal of cancer 20080315

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

  Bioorganic & medicinal chemistry letters 20080315

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

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

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

  The Biochemical journal 20080115

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

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

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

  Cancer biomarkers : section A of Disease markers 20080101

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

  Molecular cancer 20080101

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

  International journal of oncology 20071201

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

  British journal of haematology 20071101

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

  Cancer chemotherapy and pharmacology 20070701

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

  Therapeutic drug monitoring 20070401

• HDAC inhibitors and cardiac safety.

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

• 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.

  Molecular cancer therapeutics 20070101

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

  Journal of translational medicine 20070101

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

  Molecular cancer therapeutics 20060801

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

  Molecular cancer therapeutics 20030801