Veliparib (ABT-888)

Catalog No.S1004 Batch:S100417

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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
* <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.)

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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.
Targets
PARP2 [1]
(Cell-free assay)		 PARP1 [1]
(Cell-free assay)
2.9 nM(Ki) 5.2 nM(Ki)
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]
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]
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 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

Customer Product Validation

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

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

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

, , Dr.Zhang of Tianjin Medical University

Selleck's Veliparib (ABT-888) has been cited by 239 publications

Transcription-replication conflicts underlie sensitivity to PARP inhibitors [ Nature, 2024, 10.1038/s41586-024-07217-2] PubMed: 38509368
Aggregability of the SQSTM1/p62-based aggresome-like induced structures determines the sensitivity to parthanatos [ Cell Death Discov, 2024, 10(1):74] PubMed: 38346947
Thioparib inhibits homologous recombination repair, activates the type I IFN response, and overcomes olaparib resistance [ EMBO Mol Med, 2023, e16235.] PubMed: 36652375
A multi-scale map of protein assemblies in the DNA damage response [ Cell Syst, 2023, S2405-4712(23)00116-3] PubMed: 37220749
NINJ1 is activated by cell swelling to regulate plasma membrane permeabilization during regulated necrosis [ Cell Death Dis, 2023, 10.1038/s41419-023-06284-z] PubMed: 37980412
Targeting CD47-SIRPa axis shows potent preclinical anti-tumor activity as monotherapy and synergizes with PARP inhibition [ NPJ Precis Oncol, 2023, 7(1):69] PubMed: 37468567
DTX3L E3 ligase targets p53 for degradation at poly ADP-ribose polymerase-associated DNA damage sites [ iScience, 2023, 26(4):106444] PubMed: 37096048
Dynamics of endogenous PARP1 and PARP2 during DNA damage revealed by live-cell single-molecule imaging [ iScience, 2023, 26(1):105779] PubMed: 36594010
Venadaparib Is a Novel and Selective PARP Inhibitor with Improved Physicochemical Properties, Efficacy, and Safety [ Mol Cancer Ther, 2023, 22(3):333-342] PubMed: 36808277
The ATR Inhibitor VE-821 Enhances the Radiosensitivity and Suppresses DNA Repair Mechanisms of Human Chondrosarcoma Cells [ Int J Mol Sci, 2023, 24(3)2315] PubMed: 36768638

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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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