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Talazoparib | Inhibitor of PARP1, PARP2
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PARP1
  • IC 50:1.2 nM
  • IC 50:0.57 nM
  • Kd:0.29 nM
  • IC 50:1.1 nM
  • EC 50:2.5 nM
PARP2
  • Ki:0.85 nM
  • IC 50:4.1 nM
  • EC 50:2.5 nM
Inhibitor
10-100 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - PARP3 62.8 nM, PARP4 254 nM, TNKS1 322 nM, TNKS2 108 nM

Potency Assay Off-Target:
No activity was detected against PARG to 1 uM. In in vitro ADP ribosylation assays, talazoparib was ...
Selectivity Assessment Description:
No activity was detected against PARG to 1 uM. In in vitro ADP ribosylation assays, talazoparib was ...

Potency
Cellular
In Vitro

PARP1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.6b00990

PARP2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.6b00990

In Vivo Validations

Mouse
Dose: 1 mg/kg
Route of delivery: Oral
Organ of interest (O): MX-1 tumor xenograft
Target engagement assay: In MX-1 xenografts, talazoparib inhibited PAR.

DOI Reference: 10.1158/1078-0432.CCR-13-1391

Orthogonal Probes def

Olaparib
Niraparib
Veliparib

Chemical Information

Molecular Formula C19H14F2N6O
SMILEs Cn1ncnc1[C@H]1c2n[nH]c(=O)c3cc(F)cc(c23)N[C@@H]1c1ccc(F)cc1
InChI InChI=1S/C19H14F2N6O/c1-27-18(22-8-23-27)15-16(9-2-4-10(20)5-3-9)24-13-7-11(21)6-12-14(13)17(15)25-26-19(12)28/h2-8,15-16,24H,1H3,(H,26,28)/t15-,16-/m1/s1
Molecular weight 380.12 Da
AlogP 2.6285000000000007
HBond acceptors 7
HBond donors 2
Atoms 42

Vendors

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Expert Reviews

by SERP
(on 13 Apr 2017 )
Cellular Use Rating
In Model Organisms
Talazoparib is a PARP 1/2 inhibitor. This agent is an excellent tool to study PARP inhibition in both the cellular and in vivo setting.
by SERP
(on 4 May 2017 )
Cellular Use Rating
In Model Organisms
Portal staff comment: A new publication appeared in December 2016 (PMID 28001384) indicating that veliparib and niraparib are more selective than talazoparib among PARP family proteins.
by SERP
(on 15 Jun 2017 )
Cellular Use Rating
In Model Organisms
Talazoparib is an extremely potent dual PARP1/2 probe, with biochemical potencies against full length PARP1 and PARP2 slightly greater than other clinical PARP inhibitors. It's activity in BRCA1-, BRCA2-...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria