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Veliparib | Veliparib : Inhibitor of PARP1 and PARP2
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (2 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
  • Ki:5.2 nM
  • IC 50:3.3 nM
  • IC 50:5.9 nM
PARP2
  • Ki:2.9 nM
  • IC 50:17.5 nM
  • IC50:PARP 5.9 nM
Inhibitor
10-100 nM

Selectivity

In Vitro Selectivity Assessment

Potency: Ki - SIRT2 >5,000 nM

Potency Assay Off-Target:
In ADP ribosylation assays for PARP family members, veliparib was >100-fold selective for PARP1 and ...
Selectivity Assessment Description:
In ADP ribosylation assays for PARP family members, veliparib was >100-fold selective for PARP1 and ...

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? Yes

DOI Reference: 10.1021/acs.jmedchem.6b00990

In Vivo Validations

mouse, rat
Dose: 10 mg/kg (mice), 5 mg/kg (rat)
Route of delivery: Intravenous, Oral
Plasma half life: 1.6 h (mouse IV), 1.2 h (rat IV), 1.3 h (mouse oral), 1.6 h (rat oral)
Systemic clearance: 4.1 L/h/kg (mouse IV), 2.0 L/h/kg (rat IV)
Organ of interest (O): xenograft tumor, brain, plasma
Target engagement assay: Indirect: in B16F10 tumors, velaparib inhibited PAR as detected in western blot.

DOI Reference: 10.1158/1078-0432.CCR-06-3039

Orthogonal Probes def

OLAPARIB
TALAZOPARIB
NIRAPARIB

Chemical Information

Molecular Formula C13H16N4O
SMILEs C[C@]1(c2nc3cccc(C(N)=O)c3[nH]2)CCCN1
InChI InChI=1S/C13H16N4O/c1-13(6-3-7-15-13)12-16-9-5-2-4-8(11(14)18)10(9)17-12/h2,4-5,15H,3,6-7H2,1H3,(H2,14,18)(H,16,17)/t13-/m1/s1
Molecular weight 244.13 Da
AlogP 1.2604
HBond acceptors 5
HBond donors 4
Atoms 34

References

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Cross References

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Vendors

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Expert Reviews

by SERP
(on 1 Aug 2016 )
Cellular Use Rating
In Model Organisms
Veliparib is a PARP 1/2 inhibitor. This agent is an excellent tool to study PARP inhibition in both the cellular and in vivo setting. However, an important study about the mechanism of these probes...
by SERP
(on 9 Sept 2016 )
Cellular Use Rating
In Model Organisms
Velaparib is not overly potent in vivo as a a single agent but potentiates both chemo- and radiotherapy. Like other PARP inhibitors, veliparib is a potent inhibitor of PARP1 and 2 but not the other...
by SERP
(on 17 Jan 2017 )
Cellular Use Rating
Veliparib is a potent dual PARP1/2 inhibitor. It is highly recommended for studying the function of these targets in vitro. Veliparib has also shown utility in in vivo studies and even some degree of...
Veliparib is a PARP1/2 inhibitor with selectivity sufficient for cellular work to interrogate PARP1/2. While target engagement has been shown in vivo at modest doses, the lack of receptor profiling...
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