首页Chromatin/EpigeneticPARPVeliparib
Veliparib
编号 T2591     别名: ABT-888, NSC 737664
CAS 912444-00-9     分子式 C13H16N4O     分子量 244.29
靶点: PARP1; PARP2;
Veliparib (ABT-888) is an orally bioavailable inhibitor of PARP (Kis: 5.2/2.9 nM for PARP1/2). It enhances apoptosis and autophagy.
纯度:98.00%
规格 库存 单价 数量
5 mg 上海现货 518.00
10 mg 上海现货 822.00
50 mg 上海现货 2152.00
100 mg 上海现货 3672.00
200 mg 上海现货 6237.00
1 mL * 10 mM (in DMSO) 上海现货 518.00
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生物活性

产品描述

Veliparib (ABT-888) is an orally bioavailable inhibitor of PARP (Kis: 5.2/2.9 nM for PARP1/2). It enhances apoptosis and autophagy.

靶点活性

PARP1,5.2 nM (cell free)

PARP2,2.9 nM (cell free)

实验溶液

0.5% methylcellulose+0.2% Tween 80: 5 mg/mL

体外活性

Veliparib (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].

体内活性

PARP inhibition dramatically increased the efficacy of temozolomide at ABT-888 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), ABT-888 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]. ABT-888 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 ABT-888 alone, 7 days for radiation alone, and 13.5 days for combination treatment. A decrease in vitro endothelial tubule formation with ABT-888/radiation combination treatment and von Willebrand factor staining of tumor sections revealed decreased vessel formation in vivo [3].

激酶实验

PARP 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].

细胞实验

Cell 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].

动物实验

For 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].

动物模型:NCI-H460, H460, B16F10 and 9L xenografts in C57BL/6 mice

化学信息

分子量

244.29

分子式

C13H16N4O

CAS

912444-00-9

溶解度

DMSO: ≥29 mg/mL (118.7 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 4.093 ml 20.467 ml 40.935 ml
5 mM 0.819 ml 4.093 ml 8.187 ml
10 mM 0.409 ml 2.047 ml 4.093 ml
50 mM 0.082 ml 0.409 ml 0.819 ml
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