Veliparib (ABT-888)

Catalog No.S1004 Batch:S100415

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Technical Data

Formula

C13H16N4O
Molecular Weight 244.29 CAS No. 912444-00-9
Solubility (25°C)* In vitro DMSO 49 mg/mL (200.58 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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. This compound is inactive to SIRT2, increases autophagy and apoptosis, and is in Phase 3.
Targets
PARP2 [1]
(Cell-free assay)		 PARP1 [1]
(Cell-free assay)
2.9 nM(Ki) 5.2 nM(Ki)
In vitro

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

It inhibits the PARP activity with EC50 of 2 nM in C41 cells. [2]

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

It also inhibits PARP activity in H1299, DU145 and 22RV1 cells and the inhibition is independent of p53 function. At 10 μM, it suppresses the surviving fraction (SF) by 43% in the clonogenic H1299 cells. It shows effective radiosensitivity in oxic H1299 cells. Moreover, it could attenuate the SF of hypoxic-irradiated cells including H1299, DU145 and 22RV1. [4]
In vivo

Veliparib (ABT-888) has an oral bioavailability of 56%-92% in mice, Sprague-Dawley rats, beagle dogs, and cynomolgus monkeys. [1]

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

It 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]
Features Increases the efficacy of common cancer therapies such as radiation and alkylating agents.

Protocol (from reference)

Kinase Assay:

[1]
  • In vitro PARP assays

    PARP assays for Veliparib (ABT-888) 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.
Animal Study:

[1]
  • Animal Models

    NCI-H460, H460, B16F10 and 9L xenografts in C57BL/6 mice

  • Dosages

    ~25 mg/kg

  • Administration

    Orally administered

References

  • https://pubmed.ncbi.nlm.nih.gov/17473206/
  • https://pubmed.ncbi.nlm.nih.gov/19143569/
  • https://pubmed.ncbi.nlm.nih.gov/17505006/
  • http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2766769/
  • https://pubmed.ncbi.nlm.nih.gov/19934293/
  • https://pubmed.ncbi.nlm.nih.gov/17473206/
  • https://pubmed.ncbi.nlm.nih.gov/22678161/

Customer Product Validation

<p> </p><p>Number of foci detected using laser confocal microscopy and fluorescent Fluor 647 anti-H2A.X-phosphorylated (Ser139) antibody. Double-stranded breaks (red) are clearly augmented in cells incubated with 500 nmol/l of ABT-888 and 500 nmol/l of AZD-2281 compared with PBS and 1% dimethyl sulfoxide controls. Image analysis was performed using ImageJ and the ‘analyze particle’ function.</p>

Data from [ Nucl Med Commun , 2011 , 32, 1046-1051 ]

<p>Logarithmic growth curves of human Burkitt lymphoma cells over 5 days with 500 nmol/l of ABT-888 and AZD-2281 in combination with 0 Gy (a), 4 Gy (b), 8 Gy (c), and 12 Gy (d) of external beam radiation. The maximal relative reduction was 65.5% of viable cells and occurred with AZD-2281 (500 nmol/l) on day 5. DMSO, dimethyl sulfoxide.</p>

Data from [ Nucl Med Commun , 2011 , 32(11), 1046-51 ]

<p>Colorimetric poly(ADP-ribose) polymerase (PARP) activity assay showing the relative activity of the PARP-1 enzyme in Raji lymphocyte tumor cells. Results show a highly significant difference in PARP activity in the controls [PBS and dimethyl sulfoxide (DMSO)] compared with 24 h incubation with 500 nmol/l of ABT-888 and 500 nmol/l of AZD-2281. A significant increase in PARP enzyme activity is shown in DMSO-incubated cells compared with PBS control.* P < 0.05.</p>

Data from [ Nucl Med Commun , 2011 , 32(11), 1046-51 ]

<p>T47D breast cancer cells were pretreated with indicated concentrations of ABT-888</p><div><div> </div></div><p> </p>

, , Dr.Zhang of Tianjin Medical University

Selleck's Veliparib (ABT-888) Has Been Cited by 272 Publications

EXO1 as a therapeutic target for Fanconi Anaemia, ZRSR2 and BRCA1-A complex deficient cancers [ Nat Commun, 2025, 16(1):8476] PubMed: 41006228
CHD6 has poly(ADP-ribose)- and DNA-binding domains and regulates PARP1/2-trapping inhibitor sensitivity via abasic site repair [ Nat Commun, 2025, 16(1):1026] PubMed: 39863586
PARP7 inhibits type I interferon signaling to prevent autoimmunity and lung disease [ J Exp Med, 2025, 222(5)e20241184] PubMed: 39969510
Combining Multiplexed CRISPR/Cas9-Nickase and PARP Inhibitors Efficiently and Precisely Targets Cancer Cells [ Cancer Res, 2025, 10.1158/0008-5472.CAN-24-2938] PubMed: 40327605
ZNF251 haploinsufficiency confers PARP inhibitors resistance in BRCA1-mutated cancer cells through activation of homologous recombination [ Cancer Lett, 2025, 613:217505] PubMed: 39892701
Role of KLF5 in enhancing ovarian cancer stemness and PARPi resistance: mechanisms and therapeutic targeting [ J Transl Med, 2025, 23(1):492] PubMed: 40307891
Poly ADP Ribose Polymerase Inhibitors Potentiate Proton Therapy End-of-Range Effects by Accelerating Replication Forks and Promoting Transcription Conflict [ Int J Radiat Oncol Biol Phys, 2025, S0360-3016(25)06197-8] PubMed: 40882877
PARP inhibitors elicit distinct transcriptional programs in homologous recombination competent castration-resistant prostate cancer [ Mol Oncol, 2025, 10.1002/1878-0261.70098] PubMed: 40915979
Homologous Repair-Deficient Pancreatic Cancer: Refined Targeting of DNA Damage Response is an Effective Therapeutic Strategy [ United Eur Gastroent, 2025, 13(7):1328-1342] PubMed: 40823818
Tousled-like kinase loss confers PARP inhibitor resistance in BRCA1-mutated cancers by impeding non-homologous end joining repair [ Mol Med, 2025, 31(1):18] PubMed: 39844055

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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