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866323-14-0,MFCD08064035
Catalog No.:AA004OHR

866323-14-0 | Belinostat

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Purity
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1mg
98%
in stock  
$7.00   $5.00
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100mg
98%
in stock  
$37.00   $26.00
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1g
98%
in stock  
$126.00   $89.00
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  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
  • Request for Quotation
  • Download SDS
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
Technical Information
Catalog Number:
AA004OHR
Chemical Name:
Belinostat
CAS Number:
866323-14-0
Molecular Formula:
C15H14N2O4S
Molecular Weight:
318.3477
MDL Number:
MFCD08064035
SMILES:
ONC(=O)/C=C/c1cccc(c1)S(=O)(=O)Nc1ccccc1
Properties
Properties
 
Form:
Solid  
Storage:
Keep in dry area;Room Temperature;  

Computed Properties
 
Complexity:
492  
Covalently-Bonded Unit Count:
1  
Heavy Atom Count:
22  
Hydrogen Bond Acceptor Count:
5  
Hydrogen Bond Donor Count:
3  
Rotatable Bond Count:
5  
Undefined Bond Stereocenter Count:
1  
XLogP3:
1.7  

Downstream Synthesis Route

[1]Patent:WO2009/40517,2009,A2.Locationinpatent:Page/Pagecolumn54-55

[2]HelveticaChimicaActa,2005,vol.88,p.1630-1657

[3]Patent:CN105732444,2016,A.Locationinpatent:Paragraph0057;0058;0059;0060

[4]OrganicProcessResearchandDevelopment,2016,vol.20,p.1482-1488

[5]Patent:WO2017/199264,2017,A1.Locationinpatent:Page/Pagecolumn24

866323-14-0   
N-hydroxy-3-{3-(phenylamino)sulfonyphenyl}propanamide 

[1]HelveticaChimicaActa,2005,vol.88,p.1630-1657

[1]HelveticaChimicaActa,2005,vol.88,p.1630-1657

[1]SyntheticCommunications,2010,vol.40,p.2520-2524

[2]JournalofMedicinalChemistry,2011,vol.54,p.4694-4720

[3]HelveticaChimicaActa,2005,vol.88,p.1630-1657

[4]Patent:WO2018/20406,2018,A1.Locationinpatent:Page/Pagecolumn14;15

[5]Patent:WO2018/29699,2018,A1.Locationinpatent:Page/Pagecolumn16

sodium3-(1E)-3-methoxy-3-oxoprop-1-en-1-ylbenzenesulfonate 
  866323-14-0 

[1]HelveticaChimicaActa,2005,vol.88,p.1630-1657

Literature

Title: Identification of potent Yes1 kinase inhibitors using a library screening approach.

Journal: Bioorganic & medicinal chemistry letters 20130801

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: A novel histone deacetylase inhibitor, CG200745, potentiates anticancer effect of docetaxel in prostate cancer via decreasing Mcl-1 and Bcl-XL.

Journal: Investigational new drugs 20120801

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: Ovarian cancer: opportunity for targeted therapy.

Journal: Journal of oncology 20120101

Title: Histone deacetylase inhibitors globally enhance h3/h4 tail acetylation without affecting h3 lysine 56 acetylation.

Journal: Scientific reports 20120101

Title: Management of cutaneous T cell lymphoma: new and emerging targets and treatment options.

Journal: Cancer management and research 20120101

Title: Novel therapies for aggressive B-cell lymphoma.

Journal: Advances in hematology 20120101

Title: Vorinostat approved in Japan for treatment of cutaneous T-cell lymphomas: status and prospects.

Journal: OncoTargets and therapy 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: 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: 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: Phase I clinical, pharmacokinetic and pharmacodynamic study of SB939, an oral histone deacetylase (HDAC) inhibitor, in patients with advanced solid tumours.

Journal: British journal of cancer 20110301

Title: New drug therapies in peripheral T-cell lymphoma.

Journal: Expert review of anticancer therapy 20110301

Title: Histone deacetylase inhibitors in the treatment of hematological malignancies and solid tumors.

Journal: Journal of biomedicine & biotechnology 20110101

Title: Differential patterns of histone acetylation in inflammatory bowel diseases.

Journal: Journal of inflammation (London, England) 20110101

Title: Inhibition of histone deacetylases 1 and 6 enhances cytarabine-induced apoptosis in pediatric acute myeloid leukemia cells.

Journal: PloS one 20110101

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

Journal: Molecular medicine (Cambridge, Mass.) 20110101

Title: Epigenetic regulation of cancer-associated genes in ovarian cancer.

Journal: International journal of molecular sciences 20110101

Title: Zinc-chelation contributes to the anti-angiogenic effect of ellagic acid on inhibiting MMP-2 activity, cell migration and tube formation.

Journal: PloS one 20110101

Title: Interpreting clinical assays for histone deacetylase inhibitors.

Journal: Cancer management and research 20110101

Title: Autophagic and apoptotic effects of HDAC inhibitors on cancer cells.

Journal: Journal of biomedicine & biotechnology 20110101

Title: Chemotherapy in advanced bladder cancer: current status and future.

Journal: Journal of hematology & oncology 20110101

Title: Concurrent HDAC and mTORC1 inhibition attenuate androgen receptor and hypoxia signaling associated with alterations in microRNA expression.

Journal: PloS one 20110101

Title: Chromatin remodeling, cell proliferation and cell death in valproic acid-treated HeLa cells.

Journal: PloS one 20110101

Title: Romidepsin in the treatment of cutaneous T-cell lymphoma.

Journal: Journal of blood medicine 20110101

Title: Epigenomics of ovarian cancer and its chemoprevention.

Journal: Frontiers in genetics 20110101

Title: The DAC system and associations with multiple myeloma.

Journal: Investigational new drugs 20101201

Title: Targeting histone deacetyalses in the treatment of B- and T-cell malignancies.

Journal: Investigational new drugs 20101201

Title: The DAC system and associations with acute leukemias and myelodysplastic syndromes.

Journal: Investigational new drugs 20101201

Title: Histone deacetylase inhibitors: potential targets responsible for their anti-cancer effect.

Journal: Investigational new drugs 20101201

Title: Histone deacetylase inhibitors in the treatment of lymphoma.

Journal: Discovery medicine 20101101

Title: Refractory chronic lymphocytic leukemia--new therapeutic strategies.

Journal: Oncotarget 20101101

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: Targeted treatment and new agents in peripheral T-cell lymphoma.

Journal: International journal of hematology 20100701

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: Considerations for the use of plasma cytokeratin 18 as a biomarker in pancreatic cancer.

Journal: British journal of cancer 20100202

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: Histone deacetylase inhibitor therapy in epithelial ovarian cancer.

Journal: Journal of oncology 20100101

Title: Novel histone deacetylase inhibitors in clinical trials as anti-cancer agents.

Journal: Journal of hematology & oncology 20100101

Title: Response to hydralazine-valproate in a patient with mycosis fungoides.

Journal: Case reports in medicine 20100101

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20100101

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

Journal: BMC cancer 20100101

Title: Epigenomics in cancer management.

Journal: Cancer management and research 20100101

Title: New treatments for myelodysplastic syndromes.

Journal: Mediterranean journal of hematology and infectious diseases 20100101

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: Cytokeratin 18 in plasma of patients with gastrointestinal adenocarcinoma as a biomarker of tumour response.

Journal: British journal of cancer 20090804

Title: Epigenetic modifiers: basic understanding and clinical development.

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

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20090501

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: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20090301

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

Journal: International journal of cancer 20090115

Title: A phase I-II study of the histone deacetylase inhibitor valproic acid plus chemoimmunotherapy in patients with advanced melanoma.

Journal: British journal of cancer 20090113

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: A large scale shRNA barcode screen identifies the circadian clock component ARNTL as putative regulator of the p53 tumor suppressor pathway.

Journal: PloS one 20090101

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20090101

Title: New clinical developments in histone deacetylase inhibitors for epigenetic therapy of cancer.

Journal: Journal of hematology & oncology 20090101

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

Journal: International journal of oncology 20081001

Title: Histone deacetylase inhibitors as novel anticancer therapeutics.

Journal: Current oncology (Toronto, Ont.) 20081001

Title: Will histone deacetylase inhibitors require combination with other agents to fulfil their therapeutic potential?

Journal: British journal of cancer 20080902

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: Prognostic significance of the therapeutic targets histone deacetylase 1, 2, 6 and acetylated histone H4 in cutaneous T-cell lymphoma.

Journal: Histopathology 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: Epigenetic treatment of myelodysplastic syndromes and acute myeloid leukemias.

Journal: Current medicinal chemistry 20080601

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: 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: HDAC inhibitors: clinical update and mechanism-based potential.

Journal: Biochemical pharmacology 20070901

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20070501

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

Journal: Journal of translational medicine 20070101

Title: Plumb JA, et al. Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histonedeacetylase inhibitor PXD101. Mol Cancer Ther. 2003 Aug;2(8):721-8.

Title: Qian X, et al. Activity of PXD101, a histone deacetylase inhibitor, in preclinical ovarian cancer studies. Mol Cancer Ther. 2006 Aug;5(8):2086-95.

Title: Chia S, et al. Phenotype-driven precision oncology as a guide for clinical decisions one patient at a time. Nat Commun. 2017 Sep 5;8(1):435.

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