Home DNA Damage/DNA Repair PARP inhibitor - Autophagy activator - Apoptosis related activator Veliparib (ABT-888) For research use only.

Veliparib (ABT-888)

Synonyms: NSC 737664

Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis. Phase 3.

Veliparib (ABT-888) Chemical Structure

Veliparib (ABT-888) Chemical Structure

CAS No. 912444-00-9

Purity & Quality Control

Veliparib (ABT-888) Related Products

Signaling Pathway

PARP Signaling Pathways

PARP Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A4-Fuk Growth Inhibition Assay IC50=43.5691 μM SANGER
JVM-2 Growth Inhibition Assay IC50=42.9207 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=42.2538 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=41.4818 μM SANGER
HCC1187 Growth Inhibition Assay IC50=41.2771 μM SANGER
NB14 Growth Inhibition Assay IC50=40.7031 μM SANGER
SW982 Growth Inhibition Assay IC50=38.0998 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=39.3304 μM SANGER
CAL-54 Growth Inhibition Assay IC50=37.966 μM SANGER
T47D Growth Inhibition Assay IC50=37.7018 μM SANGER
H4 Growth Inhibition Assay IC50=37.567 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=36.7345 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=35.8499 μM SANGER
KG-1 Growth Inhibition Assay IC50=33.6001 μM SANGER
JVM-3 Growth Inhibition Assay IC50=35.5868 μM SANGER
MFE-280 Growth Inhibition Assay IC50=33.3889 μM SANGER
KU812 Growth Inhibition Assay IC50=32.3642 μM SANGER
COLO-684 Growth Inhibition Assay IC50=33.3599 μM SANGER
A2780 Growth Inhibition Assay IC50=30.7457 μM SANGER
RS4-11 Growth Inhibition Assay IC50=30.4241 μM SANGER
EM-2 Growth Inhibition Assay IC50=29.4901 μM SANGER
L-363 Growth Inhibition Assay IC50=29.4798 μM SANGER
MOLT-13 Growth Inhibition Assay IC50=29.3814 μM SANGER
EW-13 Growth Inhibition Assay IC50=29.3814 μM SANGER
LU-139 Growth Inhibition Assay IC50=29.3748 μM SANGER
697 Growth Inhibition Assay IC50=29.0235 μM SANGER
LB771 Growth Inhibition Assay IC50=28.8373 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=12.4663 μM SANGER
CAL-33 Growth Inhibition Assay IC50=10.434 μM SANGER
HAL-01 Growth Inhibition Assay IC50=9.8862 μM SANGER
KASUMI-1 Growth Inhibition Assay IC50=8.89266 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=8.43603 μM SANGER
C41 Kinase Assay 30 min Inhibition of PARP1 with EC50 of 0.002 μM 19888760
Jurkat Kinase Assay 96 h DMSO Inhibition of PARP1 assessed as reduction of cell viability with EC50 of 3 μM 23850199
Capan1 Growth Inhibition Assay 72 h DMSO Antiproliferative activity against BRCA2 gene mutated human Capan1 cells with IC50 of 39.7 μM 24398383
ML-1 Apoptotic Assay 2.5 μM 24 h DMSO Synergistically enhances TRAIL-induced apoptosis in ML-1 cells 24895135
HCT-116 Kinase Assay 0.5 μM 24 h PARP activity decreases 23054213
UM-SCC1 Cytotoxic Assay 10 μM 24 h Reduces the cell viability 21912620
FaDu Cytotoxic Assay 10 μM 24 h Reduces the cell viability 21912620
LoVo Function assay 30 mins Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay, EC50 = 0.00594 μM. 26652717
LoVo Function assay 30 mins Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay, EC50 = 0.00594 μM. 26652717
LoVo Function assay 30 mins Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay, EC50 = 0.00594 μM. 26652717
VC8 Cytotoxicity assay 3 days Cytotoxicity against Chinese hamster VC8 cells harboring BRCA2 deficient after 3 days by CCK8 assay, CC50 = 2.344 μM. 29335205
LoVo Cytotoxicity assay 0.4 uM 5 days Potentiation of -induced cytotoxicity in human LoVo cells assessed as GI50 at 0.4 uM after 5 days by Celltiter-Glo assay, GI50 = 6.203 μM. 26652717
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
T98G Growth Inhibition Assay IC50=44.8517 μM SANGER
BALL-1 Growth Inhibition Assay IC50=43.9532 μM SANGER
MDA-MB-361 Growth Inhibition Assay IC50=43.8414 μM SANGER
SBC-1 Growth Inhibition Assay IC50=41.3063 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=36.952 μM SANGER
BEN Growth Inhibition Assay IC50=27.9566 μM SANGER
HCC70 Growth Inhibition Assay IC50=27.7246 μM SANGER
NCI-H1693 Growth Inhibition Assay IC50=27.2898 μM SANGER
HLE Growth Inhibition Assay IC50=27.054 μM SANGER
NCI-H2029 Growth Inhibition Assay IC50=26.4238 μM SANGER
CTV-1 Growth Inhibition Assay IC50=25.8969 μM SANGER
TGBC11TKB Growth Inhibition Assay IC50=25.6863 μM SANGER
HCC1937 Growth Inhibition Assay IC50=24.746 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=23.1363 μM SANGER
A388 Growth Inhibition Assay IC50=21.9091 μM SANGER
ECC10 Growth Inhibition Assay IC50=20.7455 μM SANGER
Daoy Growth Inhibition Assay IC50=19.5649 μM SANGER
KYSE-150 Growth Inhibition Assay IC50=18.9986 μM SANGER
NKM-1 Growth Inhibition Assay IC50=18.5119 μM SANGER
H9 Growth Inhibition Assay IC50=18.2833 μM SANGER
COLO-668 Growth Inhibition Assay IC50=17.6294 μM SANGER
GP5d Growth Inhibition Assay IC50=17.053 μM SANGER
DEL Growth Inhibition Assay IC50=16.6717 μM SANGER
ChaGo-K-1 Growth Inhibition Assay IC50=16.5325 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=16.2042 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=15.9589 μM SANGER
EW-3 Growth Inhibition Assay IC50=14.5565 μM SANGER
DU-145 Growth Inhibition Assay IC50=13.9053 μM SANGER
MN-60 Growth Inhibition Assay IC50=13.5389 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=13.166 μM SANGER
HEC-1 Growth Inhibition Assay IC50=12.9196 μM SANGER
KY821 Growth Inhibition Assay IC50=12.485 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=12.4752 μM SANGER
DT40 Cytotoxic Assay 72 h DMSO Cytotoxicity against chicken BRCA2-deficient DT40 cells 24922587
PC-3 Growth Inhibition Assay 10 μM Induces a significant inhibition in colony formation  21571912
C41 Function assay Inhibition of PARP1 in human C41 cells, EC50 = 0.002 μM. 19143569
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells 29435139
EoL-1-cell Growth Inhibition Assay IC50=1.0798 μM SANGER
NCI-SNU-5 Growth Inhibition Assay IC50=3.12841 μM SANGER
BV-173 Growth Inhibition Assay IC50=5.45409 μM SANGER
HCC1806 Growth Inhibition Assay IC50=5.75173 μM SANGER
COLO-680 Growth Inhibition Assay IC50=6.21406 μM SANGER
HCC2218 Growth Inhibition Assay IC50=7.79704 μM SANGER
SK-MEL-24 Growth Inhibition Assay IC50=7.81924 μM SANGER
Mo-T Growth Inhibition Assay IC50=45.6389 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=45.7585 μM SANGER
ALL-PO Growth Inhibition Assay IC50=47.3791 μM SANGER
NCI-H510A Growth Inhibition Assay IC50=47.9034 μM SANGER
ML-2 Growth Inhibition Assay IC50=49.7856 μM SANGER
Click to View More Cell Line Experimental Data

Biological Activity

Description Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis. Phase 3.
Features Increases the efficacy of common cancer therapies such as radiation and alkylating agents.
Targets
PARP2 [1]
(Cell-free assay)		 PARP1 [1]
(Cell-free assay)
2.9 nM(Ki) 5.2 nM(Ki)
In vitro
In vitro

ABT-888 is inactive to SIRT2 (>5 μM). [1]

ABT-888 inhibits the PARP activity with EC50 of 2 nM in C41 cells. [2]

ABT-888 could decrease the PAR levels in both irradiated and nonirradiated H460 cells. ABT-888 also reduces clonogenic survival and inhibits DNA repair by PARP-1 inhibition in H460 cells. ABT-888 increases apoptosis and autophagy in H460 cells when combination with radiation. [3]

ABT-888 also inhibits PARP activity in H1299, DU145 and 22RV1 cells and the inhibition is independent of p53 function. ABT-888 (10 μM) suppresses the surviving fraction (SF) by 43% in the clonogenic H1299 cells. ABT-888 shows effective radiosensitivity in oxic H1299 cells. Furthermore, ABT-888 could attenuate the SF of hypoxic-irradiated cells including H1299, DU145 and 22RV1. [4]
Kinase Assay In vitro PARP assays
PARP assays are conducted in a buffer containing 50 mM Tris (pH 8.0), 1 mM DTT, 1.5 μM [3H]NAD+ (1.6 μCi/mmol), 200 nM biotinylated histone H1, 200 nM slDNA, and 1 nM PARP-1 or 4 nM PARP-2 enzyme. Reactions are terminated with 1.5 mM benzamide, transferred to streptavidin Flash plates, and counted using a TopCount microplate scintillation counter.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-STAT3 / STAT3 / p-AKT(S473) / p-AKT(T308) / p-ERK / p-p38 22678161
Immunofluorescence HuR BRCA1 28687616
Growth inhibition assay Cell viability (TNBC cell lines) Cell viability (melanoma cells) 27880910
In Vivo
In vivo

The oral bioavailability of ABT-888 is 56%-92% in mice, Sprague-Dawley rats, beagle dogs, and cynomolgus monkeys after oral administration. [1]

ABT-888 (25 mg/kg i.p.) could improve tumor growth delay in a NCI-H460 xenograft model with well tolerated. Combination with radiation, ABT-888 decreases the tumor vessel formation. [3]

ABT-888 reduces intratumor PAR levels by more than 95% at a dose of 3 and 12.5 mg/kg in A375 and Colo829 xenograft models and the suppression could be maintained over time. [4]
Animal Research Animal Models NCI-H460, H460, B16F10 and 9L xenografts in C57BL/6 mice
Dosages ~25 mg/kg
Administration Orally administered
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03044795 Withdrawn
Cancer
University Medical Center Groningen|AbbVie|Dutch Cancer Society
 November 2019 Phase 2
NCT02723864 Completed
Neoplasms
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
 August 9 2017 Phase 1
NCT02483104 Completed
Ovarian Cancer
AbbVie
 July 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 244.29 Formula

C13H16N4O
CAS No. 912444-00-9 SDF Download Veliparib (ABT-888) SDF
Smiles CC1(CCCN1)C2=NC3=C(C=CC=C3N2)C(=O)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 49 mg/mL ( (200.58 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

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