General
Preferred name
BELINOSTAT
Synonyms
PXD101 ()
PX105684 ()
PXD-101 ()
Belinostat (PXD101) ()
PDX-101 ()
PXD101,NSC726630, PX-105684 ()
BelinostatPXD101A-1380 ()
NSC726630 ()
PX-105684 ()
NSC-726630 ()
Beleodaq ()
(E/Z)-Belinostat ()
Rac-Belinostat ()
P&D ID
PD003512
CAS
414864-00-9
866323-14-0
Tags
available
drug
obsolete probe
Drug indication
unspecified peripheral T-cell lymphoma
Haematological malignancy
Peripheral T-cell lymphoma
Solid tumour/cancer
Drug Status
approved
investigational
Max Phase
4.0
First approval
2014
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
TOXICITY
Belinostat is genotoxic according to Ames test and may impair male fertility. Weekly complete blood count should be monitored during treatment to adjust the dosage as intravenous infusion of belinostat is frequently associated with hematologic toxicity such as leukopenia and thrombocytopenia. Incidences of infections such as sepsis, hepatotoxicity, tumor lysis syndrome, gastrointestinal toxicity, and embryo-fetal toxicity may occur. ; No specific information is available on the treatment of overdosage of Beleodaq. There is no antidote for Beleodaq and it is not known if Beleodaq is dialyzable. If an overdose occurs, general supportive measures should be instituted as deemed necessary by the treating physician.
DESCRIPTION
Belinostat is a pan-histone deacetylase (HDAC) inhibitor .
(GtoPdb)
DESCRIPTION
Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts.
PRICE
30
PRICE
46
DESCRIPTION
Rac-Belinostat (PX-105684) is a novel hydroxamic acid-type histone deacetylase (HDAC) inhibitor with antineoplastic activity. Belinostat targets HDAC enzymes, thereby inhibiting tumor cell proliferation, inducing apoptosis, promoting cellular differentiation, and inhibiting angiogenesis. This agent may sensitize drug-resistant tumor cells to other antineoplastic agents, possibly through a mechanism involving the down-regulation of thymidylate synthase.
DESCRIPTION
inhibitor of HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8
(Informer Set)
DESCRIPTION
Belinostat is a novel agent that inhibits the enzyme histone deacetylase with a sulfonamide-hydroxamide structure. It is used for the treatment of patients with relapsed or refractory peripheral T-cell lymphoma.
(Enamine Bioactive Compounds)
DESCRIPTION
Belinostat (PXD101) is an inhibitor of hydroxamic acid-type histone deacetylase (HDAC, IC50 of 27 nM in HeLa cell extracts),and with antineoplastic activity.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
24
Organisms
3
Compound Sets
24
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
ChEMBL Approved Drugs
ChEMBL Drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugMAP
Enamine Bioactive Compounds
Guide to Pharmacology
Informer Set
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
NCATS Inxight Approved Drugs
NIH Approved Oncology Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
Obsolete Compounds
Other bioactive compounds
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Welcome Trust Cancer Drugs
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
44
Molecular Weight
318.07
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
3
Rotatable Bonds
5
Ring Count
2
Aromatic Ring Count
2
cLogP
2.01
TPSA
95.5
Fraction CSP3
0.0
Chiral centers
0.0
Largest ring
6.0
QED
0.45
Structural alerts
1
historic compounds (Chemical Probes.org)
Obsolete
Related compounds
Custom attributes
(extracted from source data)
Target
HDAC1
HDAC2
HDAC3
HDAC6
HDAC8
HDAC
HDAC1, HDAC10, HDAC11, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9
Autophagy,HDAC
Compound status
clinical
Pathway
chromain histone acetylation
Autophagy
Chromatin/Epigenetic
DNA Damage/DNA Repair
Cell Cycle/DNA Damage
Epigenetics
Member status
member
MOA
HDACs
Apoptosis Inducers
Histone Deacetylase 1 (HDAC1) Inhibitors
Histone Deacetylase 2 (HDAC2) Inhibitors
Angiogenesis Inhibitors
HDAC inhibitor
Indication
peripheral T-cell lymphoma (PTCL)
Therapeutic Class
Anticancer Agents
Source data
