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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

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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