Veliparib (ABT-888)

目录号:S1004 别名: NSC 737664 中文名称:维利帕尼

仅限科研使用

Veliparib (ABT-888, NSC 737664)是一种有效的PARP1PARP2抑制剂,无细胞试验中Ki分别为5.2 nM和2.9 nM,对SIRT2没有活性。Veliparib 可增加自噬和凋亡。Phase 3。

Veliparib (ABT-888) Chemical Structure

CAS: 912444-00-9

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1277.12 现货
RMB 973.01 现货
RMB 3010.72 现货
RMB 8108.1 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Veliparib (ABT-888)发表文献205篇:

产品安全说明书

PARP抑制剂选择性比较

相关PARP产品

生物活性

产品描述 Veliparib (ABT-888, NSC 737664)是一种有效的PARP1PARP2抑制剂,无细胞试验中Ki分别为5.2 nM和2.9 nM,对SIRT2没有活性。Veliparib 可增加自噬和凋亡。Phase 3。
特性 ABT-888增强常见癌症疗法的效果,比如放射疗法和烷基化剂。
靶点
PARP2 [1]
(Cell-free assay)
PARP1 [1]
(Cell-free assay)
2.9 nM(Ki) 5.2 nM(Ki)
体外研究

ABT-888有效抑制PARP,作用于PARP-1和PARP-2时Ki值分别为5.2和2.9 nM。ABT-888降低肺癌H460细胞中克隆基因的存活率,且抑制DNA修复。[1]ABT-888抑制C41细胞,EC50为2 nM。[2] ABT-888和放射物联用减少肿瘤血管的形成。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
C41 NXfTO|A{U2mwYYPlJGF{e2G7 NHriVnk{OCCvaX6= NYi2Tnc4UW6qaXLpeIlwdiCxZjDQRXJROSC5aYToJGVEPTBib3[gNE4xODJizszN M1j2fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEi4O|YxLz5zOUi4PFc3ODxxYU6=
Jurkat M{Lz[WtqdmG|ZTDBd5NigQ>? NInmSpo6PiCq NYL6VmNkTE2VTx?= MXfJcohq[mm2aX;uJI9nKFCDUmCxJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCxZjDj[YxtKH[rYXLpcIl1gSC5aYToJGVEPTBib3[gN{DPxE1? MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh3MEG5PUc,OjN6NUCxPVk9N2F-
Capan1 M3zKZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7pfWxFPzJiaB?= NVTPSW5rTE2VTx?= MUfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFLSR2EzKGenbnWgcZV1[XSnZDDoeY1idiCFYYDhclEh[2WubIOge4l1cCCLQ{WwJI9nKDN7Lkeg{txO MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN7OEO4N{c,OjR|OUizPFM9N2F-
DT40 MU\DfZRwfG:6aXOgRZN{[Xl? Mlr3O|IhcA>? NGT0NohFVVOR M1GwcGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGOqaXPr[Y4hSlKFQUKt[IVncWOrZX70JGRVPDBiY3XscJM> MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl{MkW4O{c,OjR7MkK1PFc9N2F-
ML-1 NULzdWtoSXCxcITveIlkKEG|c3H5 NIHCPJUzNjVizszN MYOyOEBp MYLEUXNQ NF\XWG9UgW6ncnfpd5Rq[2GubImg[Y5p[W6lZYOgWHJCUUxvaX7keYNm\CCjcH;weI9{cXNiaX6gUWwuOSClZXzsdy=> M37GSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEm1NVM2Lz5{NEi5OVE{PTxxYU6=
HCT-116 MnTKT4lv[XOnIFHzd4F6 NIDk[lgxNjVizszN MoTWNlQhcA>? M3LLW3BCWlBiYXP0bZZqfHliZHXjdoVie2W| M3[z[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEW0NlE{Lz5{M{C1OFIyOzxxYU6=
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NB14 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;lPGlEPTB;NECuO|A{OSEQvF2= NHizOXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2ODZ6N{GvK|5USU6JRWK8M4E,
HCC1187 M2LVUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTRzLkK3O|Eh|ryP NFnielI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2ODZ6N{GvK|5USU6JRWK8M4E,
SBC-1 NGDaWm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vnU2lEPTB;NEGuN|A3OyEQvF2= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NFY5PzFxJ{7TRW5ITVJ:L3G+
KARPAS-45 Moq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTRzLkS4NVgh|ryP MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NFY5PzFxJ{7TRW5ITVJ:L3G+
MOLT-4 M{\jdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7jNoJKSzVyPUSyMlI2OzhizszN MmL4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVA3QDdzLze+V2FPT0WUPD;hQi=>
JVM-2 NHTlR5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfKNlRKSzVyPUSyMlkzODdizszN MnLaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVA3QDdzLze+V2FPT0WUPD;hQi=>
A4-Fuk NXP3NFhWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTR|LkW2PVEh|ryP NXzzPGVyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTB4OEexM{c,W0GQR1XSQE9iRg>?
MDA-MB-361 MojGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFy5V5pKSzVyPUSzMlg1OTRizszN NEn4eFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2ODZ6N{GvK|5USU6JRWK8M4E,
BALL-1 M3;0OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXpd4p2UUN3ME20N{46PTN{IN88US=> M3zlRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUxPjh5MT:nQnNCVkeHUkyvZV4>
T98G MoXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTR2Lki1NVch|ryP NEW5[G89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2ODZ6N{GvK|5USU6JRWK8M4E,
Mo-T M1u3TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PRSWlEPTB;NEWuOlM5QSEQvF2= MlTOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVA3QDdzLze+V2FPT0WUPD;hQi=>
MHH-PREB-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFP0fYtKSzVyPUS1Mlc2QDVizszN NICy[ZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2ODZ6N{GvK|5USU6JRWK8M4E,
ALL-PO M3TRR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTR5LkO3PVEh|ryP MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NFY5PzFxJ{7TRW5ITVJ:L3G+
NCI-H510A NGL2bpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXQWYRZUUN3ME20O{46ODN2IN88US=> NH;oXHg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2ODZ6N{GvK|5USU6JRWK8M4E,
ML-2 NUDIWVBHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkL2TWM2OD12OT63PFU3KM7:TR?= NXfpNnJbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTB4OEexM{c,W0GQR1XSQE9iRg>?
Assay
Methods Test Index PMID
Western blot p-STAT3 / STAT3 / p-AKT(S473) / p-AKT(T308) / p-ERK / p-p38 22678161
Immunofluorescence HuR BRCA1 28687616 21917757
Growth inhibition assay Cell viability (TNBC cell lines) Cell viability (melanoma cells) 27880910 29956724
体内研究 ABT-888推迟NCI-H460 移植瘤模型的肿瘤生长。ABT-888在B16F10 和9L 移植瘤模型中抑制PARP,从而增强temozolomide的抗癌活性。[1]ABT-888和其他细胞毒素药剂联用作用于MX-1移植瘤模型时显示出强抗癌效力。[2]在A375和 Colo829移植瘤模型中按肿瘤大小,每千克分别加3和12.5 mg ABT-888,可以看到肿瘤内95%以上PAR被抑制。[4]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
  • 体外PARP实验:

    在含有50 mM Tris (pH 为8.0), 1 mM DTT,和 4 mM MgCl2的缓冲溶液中进行酶活性测定。PARP反应包含1.5 μM [3H]-NAD+ (1.6 μCi/mmol), 200 nM 生物素组蛋白 H1, 200 nM slDNA,及1 nM PARP-1或4 nM PARP-2酶。在加有100 μL 反应液的 96孔板上进行SPA检测。在50 μL含有PARP和DNA的2×酶液混合物中加入50 μL 2×NAD+基底混合物,反应开始。加入150 μL 1.5 mM 苯甲酰胺反应停止。170uL反应终止液转移到链霉亲和素包被的闪熔镀层上,温育1小时,用微型板块闪烁计数器计数。

细胞实验:[2]
  • Cell lines: C41细胞
  • Concentrations: 10 μM 左右
  • Incubation Time: 0.5小时
  • Method: 在96孔板上用ABT-888处理C41细胞0.5小时。用1 mM H2O2破坏DNA10分钟,PARP被激活。用冰冻的PBS冲洗细胞,然后用预冷的甲醇/丙酮(按7:3比例混合)在−20oC下固定10 分钟。风干后,用PBS再溶解,然后用溶有5%脱脂奶粉的PBS- Tween封闭液(0.05%)在室温下阻断0.5小时。细胞和PAR抗体按1:50比例在封闭液中室温下温育1小时,然后用PBS-Tween-20冲洗5分钟,然后加入荧光素-5(6)-异硫氰酸酯 (FITC)-联用的二抗和1μg/mL DAPI封闭液中室温下温育1小时。PBS-Tween-20冲洗5分钟后,用荧光微型版计数器分析数据。
动物实验:[1]
  • Animal Models: 携带NCI-H460, H460, B16F10和9L移植瘤的C57BL/6鼠
  • Dosages: 25或3.125 mg/kg
  • Administration: 口服处理

溶解度(25°C)

体外

体内

从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
0.5% methylcellulose+0.2% Tween 80

5 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 244.29
化学式

C13H16N4O

CAS号 912444-00-9
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03044795 Withdrawn Drug: Veliparib Cancer University Medical Center Groningen|AbbVie|Dutch Cancer Society November 2019 Phase 2
NCT02723864 Completed Drug: Veliparib + VX-970 + Cisplatin Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) August 9 2017 Phase 1
NCT02483104 Completed Drug: veliparib|Drug: carboplatin|Drug: paclitaxel Ovarian Cancer AbbVie July 2015 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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