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Postion:Product Catalog >Biochemical Engineering>Inhibitors>DNA damage>PARP inhibitors>Veliparib
Veliparib
  • Veliparib

Veliparib NEW

Price $52 $74 $129
Package 5mg 10mg 25mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: Veliparib CAS No.: 912444-00-9
Purity: 99% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameVeliparib
DescriptionVeliparib (ABT-888) (ABT-888) is an orally bioavailable inhibitor of PARP (Kis: 5.2/2.9 nM for PARP1/2). It enhances apoptosis and autophagy.
Cell ResearchCell viability was quantified using the Cell Counting Kit-8 (CCK-8). This assay is based on Dojindo's highly water-soluble tetrazolium salt. WST-8 is reduced by dehydrogenases in cells to give an orange, water-soluble formazan dye. The amount of formazan dye generated by dehydrogenases in cells is directly proportional to the number of living cells. Briefly, exponentially growing HaCaT cells were seeded in 96-well plates at a density of 10,000 cells/well. 6 h or 24 h after exposure to SM and the administration of ABT-888, the CCK-8 reagent was added as recommended by the supplier [2].
Kinase AssayPARP assays were conducted in a buffer containing 50 mmol/L Tris (pH 8.0), 1 mmol/L DTT, 1.5 μmol/L [3H]NAD+ (1.6 μCi/mmol), 200 nmol/L biotinylated histone H1, 200 nmol/L slDNA, and 1 nmol/L PARP-1 or 4 nmol/L PARP-2 enzyme. Reactions were terminated with 1.5 mmol/L benzamide, transferred to streptavidin Flash plates, and counted using a TopCount microplate scintillation counter [1].
Animal ResearchFor oral pharmacokinetic studies, ABT-888 was separated from plasma and brain homogenate using liquid-liquid extraction with a mixture of ethyl acetate and hexane at alkaline pH. ABT-888 and the internal standard were separated from each other and coextracted contaminants on a 50 × 3 mm Keystone Betasil Cyano 5 μm C18 column with acetonitrile: 0.1% trifluoroacetic acid mobile phase (40:60, by volume) at a flow rate of 0.3 mL/min. Analysis was done on a Sciex API3000 Biomolecular Mass Analyzer with a turbo-ionspray interface using Sciex MacQuan software. The analysis of plasma pharmacokinetics from osmotic minipump (OMP) studies was conducted using acidified methanol precipitated plasma. Samples were injected onto a Phenomenex Synergi 4μ Polar RP column and ABT-888 eluted with a mixture of acetonitrile and 0.1% acetic acid in water at a flow rate of 0.4 mL/min. Mass analysis was done with a ThermoFinnigan LCQ Duo using Xcalibur software [1].
In vitroVeliparib (ABT-888) is a potent inhibitor of both PARP-1 and PARP-2 with K(i)s of 5.2 and 2.9 nmol/L, respectively [1]. In the HaCaT cell model, ABT-888 can reduce SM-induced NAD(+)/ATP depletion and apoptosis/necrosis [2]. ABT-888 reduced clonogenic survival in H460 lung cancer cells and inhibited DNA repair as shown by enhanced expression of DNA strand break marker histone gamma-H2AX [3].
In vivoPARP inhibition dramatically increased the efficacy of temozolomide at Veliparib doses as low as 3.1 mg/kg/d and a maximal efficacy achieved at 25 mg/kg/d. In the MX-1 breast xenograft model (BRCA1 deletion and BRCA2 mutation), Veliparib potentiated cisplatin, carboplatin, and cyclophosphamide, causing regression of established tumors, whereas, with comparable doses of cytotoxic agents alone, only modest tumor inhibition was exhibited [1]. Veliparib increased tumor growth delay at well-tolerated doses in murine models. For a 5-fold increase in tumor volume, tumor growth delay was 1 day for Veliparib alone, 7 days for radiation alone, and 13.5 days for combination treatment. A decrease in vitro endothelial tubule formation with Veliparib/radiation combination treatment and von Willebrand factor staining of tumor sections revealed decreased vessel formation in vivo [3].
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationH2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 50 mg/mL (204.67 mM)
KeywordsVeliparib | inhibit | PARP | Inhibitor | ABT 888 | Autophagy | NSC737664 | poly ADP ribose polymerase | ABT888 | NSC-737664
Inhibitors RelatedHydroxychloroquine | Guanidine hydrochloride
Related Compound LibrariesBioactive Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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