General
Preferred name
TALAZOPARIB
Synonyms
BMN-673 ()
TALAZOPARIB TOSYLATE ()
LT-673 ()
BMN673ts ()
BMN 673ts ()
BICALUTAMIDE ()
Talazoparib (BMN 673) ()
PF-06944076 ()
BMN 673 ()
BMN-673TS ()
TALZENNA ()
Talazoparib tosilate ()
P&D ID
PD010641
CAS
1207456-01-6
1373431-65-2
Tags
available
probe
drug
Approved by
EMA
FDA
First approval
2018
Drug indication
Breast cancer
Psoriatic arthritis
breast neoplasm
triple-negative breast cancer
Drug Status
approved
investigational
Max Phase
4.0
Probe info
Probe type
P&D approved
experimental probe
Probe selectivity
family-selective
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
9
No orthogonal probes found
Similar probes
2
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
Talazoparib is clastogenic due to its pharmacological mechanism [FDA Label]. Talazoparib does not appear to be mutagenic and no data is available on carcinogenicity. ; ; In repeat-dose toxicity studies up to 3-months duration at doses â¥0.04 mg/kg/day in rats and â¥0.01 mg/kg/day in dogs resulted in decreased organ weights, luminal cellular debris, reduced sperm, and degeneration/atrophy in the testis and epididymis [FDA Label]. These doses were equivalent to approximately 1.0 times and 0.2 times normal human exposure. Follicular atresia of the ovary was observed in rats at doses â¥1 mg/kg/day, equivalent to 9.5 times normal human exposure. While no fertility data exists these results suggest a potential for reduced fertility due to talazoparib exposure.
DESCRIPTION
Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity[1].
PRICE
69
DESCRIPTION
Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC50 of 0.57 nM for PARP1.
PRICE
84
MOA
Inhibitor
(Chemical Probes.org)
DESCRIPTION
Talazoparib (LT-673) is a new-type PARP inhibitor (IC50: 0.58 nM), It similarly binds to PARP1/2 (Kis: 1.2/0.85 nM).
(TargetMol Bioactive Compound Library)
DESCRIPTION
Talazoparib tosylate (BMN 673ts) is an orally active and highly potent PARP1/2 inhibitor with antitumor activity for the study of specific breast cancers.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
13
Organisms
0
Compound Sets
25
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
Chemical Probes.org
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
EU-OPENSCREEN Bioactive Compound Library
High-quality chemical probes
LSP-MoA library (Laboratory of Systems Pharmacology)
Mcule NIBR MoA Box Subset
NCATS Inxight Approved Drugs
NIH Approved Oncology Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
Selleckchem Bioactive Compound Library
Welcome Trust Cancer Drugs
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
44
Molecular Weight
380.12
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
2
Rotatable Bonds
2
Ring Count
5
Aromatic Ring Count
4
cLogP
2.63
TPSA
88.49
Fraction CSP3
0.16
Chiral centers
2.0
Largest ring
6.0
QED
0.56
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Pathway
Genome integrity
Cell Cycle/DNA Damage
Epigenetics
Chromatin/Epigenetic
DNA Damage/DNA Repair
Target
PARP1, PARP2
PARP
PARP1
PARP2
Member status
member
MOA
Inhibitor of PARP1 and PARP2
PARP inhibitor
Indication
breast cancer
Therapeutic Class
Poly (ADP-ribose) polymerase (PARP) inhibitor
Target class
Other post-translational modification, Other post-translational modification
Target subclass
PARP, PARP
Source data
