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Chemical Structure| 866323-14-0 Chemical Structure| 866323-14-0

Structure of Belinostat
CAS No.: 866323-14-0

Chemical Structure| 866323-14-0

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Belinostat (PXD101; PX105684) displays potent inhibition of HDAC, with an IC50 of 27 nM in HeLa cell extracts.

Synonyms: PXD101; PX105684; NSC726630

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Product Details of Belinostat

CAS No. :866323-14-0
Formula : C15H14N2O4S
M.W : 318.34
SMILES Code : O=C(NO)/C=C/C1=CC=CC(S(=O)(NC2=CC=CC=C2)=O)=C1
Synonyms :
PXD101; PX105684; NSC726630
MDL No. :MFCD08064035
InChI Key :NCNRHFGMJRPRSK-MDZDMXLPSA-N
Pubchem ID :6918638

Safety of Belinostat

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Belinostat

epigenetics

Isoform Comparison

Biological Activity

Target
  • HDAC

    HDAC, IC50:27 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
resting memory CD4 T cells 400 nM 14 days To evaluate the efficiency of Belinostat in reversing HIV-1 latency, results showed that Belinostat effectively induced HIV-1 replication, and the induced virus was not only replication competent but also infectious. PMC4733986
HT29 colon cancer cells 2 μM 24 h To evaluate the effects of Belinostat on cell proliferation and metabolism, results showed that Belinostat significantly inhibited the proliferation of HT29 cells and increased phosphocholine (PC) levels. PMC3378496
PC3 prostate cancer cells 0.9 μM 24 h To evaluate the effects of Belinostat on cell proliferation and metabolism, results showed that Belinostat significantly inhibited the proliferation of PC3 cells and increased phosphocholine (PC) levels. PMC3378496
SW579 cells 1 µM 24 h Belinostat at a concentration of 1 µM for 24 h significantly induced cell death in SW579 cells, with a dead/live cell ratio of 120%. PMC6359659
Lung squamous cell carcinoma cells 0.1, 0.2, 0.3, 1, 3 µM 72 h To determine the sensitivity of Belinostat in lung squamous cell carcinoma cells, the results showed that Belinostat exhibited differential sensitivities in different cell lines and induced apoptosis. PMC5537703

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice HT29 colon cancer xenograft model Oral 60 mg/kg Once daily for 3 days To evaluate the effects of Belinostat on tumor growth and metabolism, results showed that Belinostat significantly inhibited the growth of HT29 tumors and increased phosphocholine (PC) levels. PMC3378496
SCID mice Calu-1 xenograft model Oral 40 mg/kg 5 days a week for 3 weeks To evaluate the antitumor activity of Belinostat in the Calu-1 xenograft model, the results showed that Belinostat alone or in combination with cisplatin did not exhibit significant antitumor activity. PMC5537703

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00865969 Peripheral T-cell Lymphoma PHASE2 COMPLETED 2014-10-27 City of Hope National Medical ... More >>Center, Duarte, California, 91010, United States|Wilshire Oncology Medical Group, Inc, La Verne, California, 91750, United States|Comprehensive Cancer Center, Palm Springs, California, 92262, United States|Yale Cancer Center-Section of Medical Oncology, New Haven, Connecticut, 06520, United States|Oncology Associates of Bridgeport, Trumbull, Connecticut, 06611, United States|Boca Raton Clinical Research Associates, Boca Raton, Florida, 33432, United States|Georgia Health Sciences University, Augusta, Georgia, 30912-3125, United States|Northwestern University, Chicago, Illinois, 60611, United States|Rush University Medical Center, Chicago, Illinois, 60612, United States|Kellogg Cancer Care Center, Evanston, Illinois, 60201, United States|Illinois Cancer Specialists/Cancer Care & Hematology Specialists of Chicagoland, Niles, Illinois, 60714, United States|Illinois CancerCare, P.C., Peoria, Illinois, 61615, United States|Center for Cancers and Blood Disorders, Bethesda, Maryland, 20817, United States|Dana Farber Cancer Institute, Boston, Massachusetts, 02115, United States|Boston University Medical Center, Boston, Massachusetts, 02118, United States|Karmanos Cancer Institute, Detroit, Michigan, 48201, United States|Henry Ford Health System, Detroit, Michigan, 48202, United States|Saint Louis University, Saint Louis, Missouri, 63110, United States|Washington University School of Medicine, Saint Louis, Missouri, 63110, United States|Northern New Jersey Cancer Associates, Hackensack, New Jersey, 07601, United States|Morristown Memorial Hospital, Morristown, New Jersey, 07962, United States|Bronx River Medical Associates, PC, Bronx, New York, 10467, United States|Erie County Medical Center (Roswell Park), Buffalo, New York, 14215, United States|Monter Cancer Center, Lake Success, New York, 11067, United States|New York University Cancer Institute, New York, New York, 10016, United States|New York University, New York, New York, 10016, United States|Memorial Sloan-Kettering Cancer Center, New York, New York, 10021, United States|Upstate Medical Univeristy Syracuse, Syracuse, New York, 13210, United States|Duke University Medical Center, Durham, North Carolina, 27710, United States|Hematology Associates, Bedford, Ohio, 44146, United States|St Luke's Cancer Center, Bethlehem, Pennsylvania, 18015, United States|Penn State Hershey Cancer Institute, Hershey, Pennsylvania, 17033, United States|Fox Chase Cancer Center, Philadelphia, Pennsylvania, 19111, United States|Avera Cancer Center, Sioux Falls, South Dakota, 57105, United States|Associates In Oncology and Hematology, Chattanooga, Tennessee, 37421, United States|University of Tennessee Cancer Institute, Knoxville, Tennessee, 37920, United States|Accelerated Community Oncology Reseaerch Network, Inc. (ACORN), Memphis, Tennessee, 38138, United States|UT - M. D. Anderson Cancer Center, Houston, Texas, 77030, United States|The UT Health Science Centre at San Antonio, San Antonio, Texas, 78229, United States|Massey Cancer Center, Richmond, Virginia, 23298-0035, United States|Cascade Cancer Center, Kirkland, Washington, 98304, United States|Fred Hutchinson Cancer Research Center - Seattle Cancer Care Alliance, Seattle, Washington, 98109, United States|ZNA Middelheim, Antwerpen, 2020, Belgium|ZNA Stuivenberg, Antwerpen, 2060, Belgium|Clinique Universitaire Saint Luc, Service Hématologie, Bruxelles, 1200, Belgium|AZ St. Jan, Brügge, 8000, Belgium|Universitair Ziekenhuis Gent, Gent, 9000, Belgium|University of Liege, Divisions of Hematology and Medical Oncology, Liege, 4000, Belgium|Cliniques Universitaires UCL Mont Godinne, Service Hématologie, Yvoir, 5530, Belgium|University of British Columbia, Vancouver, British Columbia, V5Z 4E6, Canada|CHA H?pital de l'Enfant-Jésus, Quebec City, Quebec, G1J1Z4, Canada|McGill University, Montreal, H2W1S6, Canada|CHC Split Clinic of Internal Diseases, Split, 21000, Croatia|CHC Zagreb Clinic of Internal Diseases, Zagreb, 10000, Croatia|UH Dubrava Clinic of Internal Diseases, Zagreb, 10000, Croatia|CHC Rijeka, Clinic of Internal Diseases, Zagreb, 1000, Croatia|H:S Rigshospitalet, The Finsen Centre, KAT, Haematology Department 4241, Copenhagen, 2100, Denmark|H?pital de l'Archet, Centre Hospitalier Universitaire (CHU) de Nice, Hématologie Clinique, Nice, 6202, France|Groupe Hospitalier Sud Réunion, Site Saint-Pierre, Saint-Pierre Cedex, 97448, France|Klinik Essen Süd, Evangelisches Krankenhaus, Essen, 45239, Germany|Leitender Oberarzt/Klinik für Onkologie und H?matologie, Frankfurt, 60488, Germany|Universit?t G?ttingen, Abteilung H?matologie und Onkologie, G?ttingen, 37075, Germany|Universit?tsklinikum (A?R) der Martin-Luther-Universit?t Halle-Wittenberg, Halle, 06120, Germany|Asklepios Klinik St. Georg, Hamburg, 20099, Germany|Universit?tsklinikum des Saarlandes, Homburg/Saar, 66424, Germany|Universit?tsklinikum Leipzig A?R, Leipzig, 04103, Germany|Universit?tsmedizin der johannes Gutenberg -Universit?t Mainz, Mainz, 55131, Germany|University Hospital Marburg, Marburg, 35043, Germany|Münchner Studienzentrum Klinikum Rechts der Isar, München, 81675, Germany|Klinikum Nuernberg Nord, Nuernberg, 90419, Germany|Universit?tsklinikum Rostock, Rostock, 18057, Germany|Universit?tsklinikum Ulm, Ulm, 89081, Germany|Szt István és Szt. Laszlo, Budapest, 1097, Hungary|Belgyógyászati Klinika, Debrecen, 4032, Hungary|Belgyógyászati Klinika Gy?r, Gy?r, 9042, Hungary|Belgyógyászati Klinika es Kardiologial K?zpont, Szeged, 6720, Hungary|The Soroka University Medical Center, Beer Sheva, 84101, Israel|Rambam Medical Center Department of Hematology, Haifa, 31096, Israel|Hadassah University Hospital Sharet Building Department of Hematology, Jerusalem, 91120, Israel|Rabin Medical Center Belinson Campus, Petach Tikva, 49100, Israel|Ospedale Sant'Orsola, Instituto di Ematologia e Oncologia Medica, Bologna, 40138, Italy|Ospedale Policlinico Careggi, Firenze, 50134, Italy|VU Medical Center, Department of Haematology, Amsterdam, 7081 HV, Netherlands|University Medical Center Groningen UMCG, Department of Haematologie, Groningen, 9700, Netherlands|Erasmus University Medical Center, Rotterdam, 3015, Netherlands|Isala Clinics, Department of Haematololgy, Zwolle, 8025 AB, Netherlands|Klinika Nowotworów Ukladu Chlonnego Centrum Onkologii Instytut Marii Sklodowskiej-Curie, Warszawa, Mazowieckie, 02-781, Poland|Uniwersyteckie Centrum Kliniczne Klinika Hematologii i Transplantologii, Gdansk, 80-952, Poland|Ma?opolskie Centrum Medyczne, Kraków, 30-510, Poland|Szpital Wojewódzki w Opolu/Oddzia? Hematologii, Opole, 45-051, Poland|MTZ Clinical Research Sp z o.o., Warszawa, 02-106, Poland|Instytut Hematologii i Transfuzjologii Klinika Hematologii, Warszawa, 02-776, Poland|Wojskowy Instytut Medyczny Klinika Chorób/Wewn?trznych i Hematologii Centralnego Szpitala, Warszawa, 04-141, Poland|Wojewódzki Szpital Specjalistyczny im M. Kopernika w ?odzi Oddzia? Hematologii - Klinika Hematologii, ?ód?, 93-510, Poland|State Therapeutical and Prophylactic Institution Chelyabinsk Regional Clinical Oncology Dispensary, Chelyabinsk, 454087, Russian Federation|Russian Cancer Research Centre named after N.N. Blokhin of Russian Academy of Medical Sciences, Moscow, 115478, Russian Federation|Research Center of Haematology, Moscow, 125167, Russian Federation|Narodny Onkologicky Ustav (NOU), Bratislava, 83310, Slovakia|Klinika Hematologie a Onkohematologie FNLP a LF UPJS, Kosice, 04066, Slovakia|Tygerberg Hospital, Department of Radiation Oncology, Bellville, 7505, South Africa|Drs pirjol, Szpak and Moodley Inc., Durban, 4126, South Africa|Medical Oncology 2nd Floor Radiotherapy building Steve Biko Academic Hospital, Pretoria, 0002, South Africa|Pretoria Academic Hospital, Department of Radiation Oncology, Pretoria, 0002, South Africa|Complexo Hospitalario a Coruna, A Coruna, 15006, Spain|Hospital Clinico Universitario de Santiago, A Coru?a, 15706, Spain|ICO Hospital Germans Trias i Pujol, Badalona, 08918, Spain|Hospital Duran i Reinals, Barcelona, 08007, Spain|Hospital Universitario Virgen de la Arrixaca, El Palmar, 30120, Spain|Hospital General Universitario Gregorio Maranón, Madrid, CP 28007, Spain|Hospital Universitario Morales Meseguer, Murcia, 30008, Spain|Hospital Universitario Central de Asturias, Oviedo, 33006, Spain|St James's Institute of Oncology Bexley Wing, Leeds, LS9 7TF, United Kingdom|Leicester Royal Infirmary, Leicester, LE1 5WW, United Kingdom|Institute of Cancer/ Centre for Medical Oncology/Barts and The London School of Medicine and Dentistry, London, EC1A 7BE, United Kingdom|The Christie NHS Foundation Trust, The Christie Hospital,, Manchester, M20 4BX, United Kingdom|Northern Centre for Cancer Care, Freeman Hospital, Newcastle Upon Tyne, NE7 7DN, United Kingdom|The Royal Marsden Haemato-Oncology Wards, Sutton, SM2 5PT, United Kingdom Less <<
NCT00431340 Multiple Myeloma PHASE2 TERMINATED 2025-06-07 Oncotherapeutics, West Hollywo... More >>od, California, 90069, United States|Center for cancer and blood disorders, Bethesda, Maryland, 20817, United States|Baylor University Medical Center, Dallas, Texas, 75246, United States Less <<
NCT01583777 Advanced Cancer PHASE1 COMPLETED 2025-04-15 Hospital Universitario Madrid ... More >>Sanchinarro, Madrid, 28050, Spain Less <<
NCT02679131 Relapsed/Refractory Solid Tumo... More >>rs/Hematological Malignancies Less << PHASE1 TERMINATED 2025-06-17 Innovative Clinical Research I... More >>nstitute, Whittier, California, 90603, United States|Gabrail Cancer Center Research, Canton, Ohio, 44718, United States Less <<
NCT01273155 Neoplasms|Lymphomas PHASE1 COMPLETED 2017-10-25 University of California, Davi... More >>s, Davis, California, 95616, United States|City of Hope National Medical Center, Duarte, California, 91010, United States|USC Norris Cancer Center, Los Angeles, California, 90033, United States|Emory University, Atlanta, Georgia, 30322-1102, United States|National Institutes of Health Clinical Center, 9000 Rockville Pike, Bethesda, Maryland, 20892, United States|Karmanos Cancer Institute, Detroit, Michigan, 48201, United States|Albert Einstein College of Medicine, Bronx, New York, 10461, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.14mL

0.63mL

0.31mL

15.71mL

3.14mL

1.57mL

31.41mL

6.28mL

3.14mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

[1]Yoon S, Eom GH, et al. HDAC and HDAC Inhibitor: From Cancer to Cardiovascular Diseases. Chonnam Med J. 2016 Jan;52(1):1-11.

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

[3]Sawas A, Radeski D, et al. Belinostat in patients with refractory or relapsed peripheral T-cell lymphoma: a perspective review. Ther Adv Hematol. 2015 Aug;6(4):202-8.

[4]Dai Y, Chen S, et al. Interactions between bortezomib and romidepsin and belinostat in chronic lymphocytic leukemia cells. Clin Cancer Res. 2008 Jan 15;14(2):549-58.

[5]Mottamal M, Zheng S, et al. Histone deacetylase inhibitors in clinical studies as templates for new anticancer agents. Molecules. 2015 Mar 2;20(3):3898-941.

[6]New M, Olzscha H, et al. HDAC inhibitor-based therapies: can we interpret the code? Mol Oncol. 2012 Dec;6(6):637-56.

[7]Qian X, Ara G, et al. Activity of the histone deacetylase inhibitor belinostat (PXD101) in preclinical models of prostate cancer. Int J Cancer. 2008 Mar 15;122(6):1400-10.

[8]Buckley MT, Yoon J, et al. The histone deacetylase inhibitor belinostat (PXD101) suppresses bladder cancer cell growth in vitro and in vivo. J Transl Med. 2007 Oct 12;5:49.

[9]Warren KE, McCully C, et al. Plasma and cerebrospinal fluid pharmacokinetics of the histone deacetylase inhibitor, belinostat (PXD101), in non-human primates. Cancer Chemother Pharmacol. 2008 Aug;62(3):433-7. Epub 2007 Oct 25.

 

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