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Veliparib

产品编号 T2591 CAS 912444-00-9

别名: ABT-888, NSC 737664, 维利帕尼

Veliparib (ABT-888) 是一种可口服的 PARP 抑制剂，抑制PARP1和PARP2的Ki 分别为 5.2 和 2.9 nM。它增强细胞凋亡和自噬。

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Veliparib, CAS 912444-00-9

规格	价格/CNY	货期
1 mg	￥ 209	现货
5 mg	￥ 469	现货
10 mg	￥ 728	现货
25 mg	￥ 1,180	现货
50 mg	￥ 1,730	现货
100 mg	￥ 3,230	现货
200 mg	￥ 4,770	现货
500 mg	￥ 7,530	现货
1 mL * 10 mM (in DMSO)	￥ 519	现货

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其他形式的 Veliparib:

Veliparib dihydrochloride
现货

选择批次

纯度: 99.76%

纯度: 99%

纯度: 98.92%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Veliparib (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.
靶点活性	PARP2:2.9 nM (cell free), PARP1:5.2 nM (cell free)
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].

别名	ABT-888, NSC 737664, 维利帕尼
分子量	244.29
分子式	C13H16N4O
CAS No.	912444-00-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 29 mg/mL(118.7 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	4.0935 mL	20.4675 mL	40.935 mL	102.3374 mL
	5 mM	0.8187 mL	4.0935 mL	8.187 mL	20.4675 mL
	10 mM	0.4093 mL	2.0467 mL	4.0935 mL	10.2337 mL
	20 mM	0.2047 mL	1.0234 mL	2.0467 mL	5.1169 mL
	50 mM	0.0819 mL	0.4093 mL	0.8187 mL	2.0467 mL
	100 mM	0.0409 mL	0.2047 mL	0.4093 mL	1.0234 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

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参考文献

1. Donawho CK, et al. ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models. Clin Cancer Res. 2007 May 1;13(9):2728-37. 2. Liu F, et al. Effects of poly (ADP-ribose) polymerase-1 (PARP-1) inhibition on sulfur mustard-induced cutaneous injuries in vitro and in vivo. PeerJ. 2016 Apr 4;4:e1890. 3. Albert JM, et al. Inhibition of poly(ADP-ribose) polymerase enhances cell death and improves tumor growth delay in irradiated lung cancer models. Clin Cancer Res. 2007 May 15;13(10):3033-42. 4. Mao K, Chen J, Yu H, et al. Poly (ADP‐ribose) polymerase 1 inhibition prevents neurodegeneration and promotes α‐synuclein degradation via transcription factor EB‐dependent autophagy in mutant α‐synucleinA53T model of Parkinson's disease[J]. Aging Cell. 2020: e13163. 5. Epub 2020 May 31. PARP1 inhibition prevents neurodegeneration and promotes α-synuclein degradation via TFEB-dependent autophagy in mutant α-synucleinA53T model of Parkinson's disease. aging cell. 2020 Jun;19(6):e13163

文献引用

1. Kanmin Mao,Jialong Chen,Honglin Yu,Huihui Li,Yixian Ren. Poly (ADP-ribose) polymerase 1 inhibition prevents neurodegeneration and promotes α-synuclein degradation via transcription factor EB-dependent autophagy in mutant α-synucleinA53T model of Parkinson's disease. Aging Cell. 2020 Jun;19(6):e13163 2. Epub 2020 May 31 PARP1 inhibition prevents neurodegeneration and promotes α-synuclein degradation via TFEB-dependent autophagy in mutant α-synucleinA53T model of Parkinson's disease. aging cell. 2020 Jun;19(6):e13163 3. Wang J, Xing W, Lin Y, et al. Blocking PARP activity with the inhibitor veliparib enhances radiotherapy sensitivity in endometrial carcinoma. Journal of Clinical Laboratory Analysis. 2022: e24435

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Veliparib 912444-00-9 Autophagy Chromatin/Epigenetic DNA Damage/DNA Repair PARP ABT-888 inhibit Inhibitor NSC 737664 ABT 888 NSC737664 维利帕尼 poly ADP ribose polymerase ABT888 NSC-737664 inhibitor

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

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Veliparib

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords