维利帕尼|T2591|TargetMol

Veliparib
912444-00-9

￥209 1mg 起订

￥469 5mg 起订

￥728 10mg 起订

上海更新日期：2024-12-02

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产品详情:

中文名称：: 维利帕尼

英文名称：: Veliparib

CAS号：: 912444-00-9

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99%

产品类别：: 抑制剂

货号：: T2591

Product Introduction

Bioactivity

名称	Veliparib
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.
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].
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].
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].
体外活性	Veliparib (ABT-888) 是一种针对PARP-1和PARP-2的高效抑制剂，其K(i)分别为5.2和2.9 nmol/L [1]。在HaCaT细胞模型中，ABT-888能减少SM诱导的NAD(+)/ATP耗竭以及凋亡/坏死[2]。ABT-888减少了H460肺癌细胞的集落形成能力，并通过DNA链断裂标志物组蛋白γ-H2AX表达的增强，抑制了DNA修复[3]。
体内活性	PARP抑制剂显著提高了以Veliparib剂量低至3.1 mg/kg/d时的temozolomide效能，并在25 mg/kg/d时达到最大效能。在MX-1乳腺异种移植模型（BRCA1缺失和BRCA2突变）中，Veliparib增强了cisplatin、carboplatin和cyclophosphamide的效果，导致已建立肿瘤的缩小；而与单独相当剂量的细胞毒性化合物相比，只展现出适度的肿瘤抑制作用[1]。在小鼠模型中，Veliparib在耐受剂量下增加了肿瘤生长延迟。对于肿瘤体积增加5倍，Veliparib单独使用的肿瘤生长延迟为1天，仅辐射治疗为7天，而联合治疗为13.5天。体外Veliparib/辐射联合治疗减少了内皮管腔形成，而体内通过von Willebrand因子染色的肿瘤切片显示出血管形成的减少[3]。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 50 mg/mL (204.67 mM)
关键字	Veliparib \| inhibit \| PARP \| Inhibitor \| ABT 888 \| Autophagy \| NSC737664 \| poly ADP ribose polymerase \| ABT888 \| NSC-737664
相关产品	Guanidine hydrochloride \| Naringin \| Valproic Acid \| Taurine \| Gefitinib \| Aceglutamide \| Hydroxychloroquine \| Curcumin \| Stavudine \| Salicylic acid \| Paeonol \| Sodium 4-phenylbutyrate
相关库	抑制剂库 \| 经典已知活性库 \| 已知活性化合物库 \| 抗衰老化合物库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库 \| 抗癌药物库

维利帕尼|||NSC 737664|||ABT-888|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子