Veliparib (ABT-888)

For research use only. Not for use in humans.

目录号:S1004 别名: NSC 737664 中文名称:维利帕尼

Veliparib (ABT-888) Chemical Structure

CAS No. 912444-00-9

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。

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 1859.13 现货
RMB 3010.72 现货
RMB 8108.1 现货
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客户使用Selleck生产的Veliparib (ABT-888)发表文献189篇:

产品安全说明书

PARP抑制剂选择性比较

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 MVXLbY5ie2ViQYPzZZk> M4TJTVMxKG2rbh?= Mn7oTY5pcWKrdHnvckBw\iCSQWLQNUB4cXSqIFXDOVAhd2ZiMD6wNFIh|ryP MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh6OEe2NEc,OTl6OEi3OlA9N2F-
Jurkat NWnaWm9xU2mwYYPlJGF{e2G7 MY[5OkBp M1XHTmROW09? MoLCTY5pcWKrdHnvckBw\iCSQWLQNUBie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gZ4VtdCC4aXHibYxqfHlid3n0bEBGSzVyIH;mJFMh|ryP MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh3MEG5PUc,OjN6NUCxPVk9N2F-
Capan1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYe3NkBp M2rKNWROW09? Mn;URY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDCVmNCOiCpZX7lJI12fGG2ZXSgbJVu[W5iQ3HwZY4yKGOnbHzzJJdqfGhiSVO1NEBw\iB|OT63JO69VQ>? MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN7OEO4N{c,OjR|OUizPFM9N2F-
DT40 MWXDfZRwfG:6aXOgRZN{[Xl? MkfzO|IhcA>? M3eybWROW09? NWrDbmdlS3m2b4TvfIlkcXS7IHHnZYlve3RiY3jpZ4tmdiCEUlPBNk1l\W[rY3nlcpQhTFR2MDDj[Yxtew>? M{LSXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUKyOVg4Lz5{NEmyNlU5PzxxYU6=
ML-1 NX;PUG1sSXCxcITveIlkKEG|c3H5 MWCyMlUh|ryP NISy[pMzPCCq MXjEUXNQ NI\sbXZUgW6ncnfpd5Rq[2GubImg[Y5p[W6lZYOgWHJCUUxvaX7keYNm\CCjcH;weI9{cXNiaX6gUWwuOSClZXzsdy=> Mm\WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OUWxN|UoRjJ2OEm1NVM2RC:jPh?=
HCT-116 MoW1T4lv[XOnIFHzd4F6 NWnQSldKOC53IN88US=> NFPEXnEzPCCq NYX6e3ZmWEGUUDDhZ5Rqfmm2eTDk[YNz\WG|ZYO= M1H0dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEW0NlE{Lz5{M{C1OFIyOzxxYU6=
UM-SCC1 MnPYR5l1d3SxeHnjJGF{e2G7 NGnOWpAyOCEQvF2= NWH4N4dzOjRiaB?= NVnrSIhwWmWmdXPld{B1cGViY3XscEB3cWGkaXzpeJk> NXfyNGd7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5NVI3OjBpPkKxPVEzPjJyPD;hQi=>
FaDu MkDYR5l1d3SxeHnjJGF{e2G7 MUixNEDPxE1? MXyyOEBp MVvS[YR2[2W|IITo[UBk\WyuII\pZYJqdGm2eR?= MnjtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7MUK2NlAoRjJzOUGyOlIxRC:jPh?=
PC-3 NIDEN5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;KNVAh|ryP NEH4[ZhKdmS3Y3XzJIEhe2mpbnnmbYNidnRiaX7obYJqfGmxbjDpckBkd2yxbomg[o9zdWG2aX;uxsA> MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5MUmxNkc,OjF3N{G5NVI9N2F-
C41 NGj2N2NHfW6ldHnvckBie3OjeR?= NIX5b5VKdmirYnn0bY9vKG:oIGDBVnAyKGmwIHj1cYFvKEN2MTDj[YxteyxiRVO1NEA:KDBwMECyJO69VS5? Mn3KQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTlzNEO1OlkoRjF7MUSzOVY6RC:jPh?=
LoVo NX3hT3hZTnWwY4Tpc44h[XO|YYm= MYGzNEBucW6| M2jJZWlvcGmkaYTpc44hd2ZiUFHSVEBqdiCqdX3hckBNd1[xIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YheG:ueTjBSHAqNXKrYn;z[UBxd2y7bXXybZpifGmxbjDmc5IhOzBibXnud{BjgSCobIXvdoV{[2WwY3WgZZN{[XluIFXDOVAhRSByLkCwOVk1KM7:TT6= M1\C[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyO|E4Lz5{Nk[1NlcyPzxxYU6=
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HCC1187 NET2b3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M335[WlEPTB;NEGuNlc4OSEQvF2= Ml;SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVA3QDdzLze+V2FPT0WUPD;hQi=>
SBC-1 MoXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\5ZmxmUUN3ME20NU4{ODZ|IN88US=> M{G5eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUxPjh5MT:nQnNCVkeHUkyvZV4>
KARPAS-45 M{jUc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrUTVA6UUN3ME20NU41QDF6IN88US=> M2PG[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUxPjh5MT:nQnNCVkeHUkyvZV4>
MOLT-4 MlfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfwOHZKSzVyPUSyMlI2OzhizszN NELicIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2ODZ6N{GvK|5USU6JRWK8M4E,
JVM-2 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vJNmlEPTB;NEKuPVIxPyEQvF2= Mn7qQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVA3QDdzLze+V2FPT0WUPD;hQi=>
A4-Fuk Mlv2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTR|LkW2PVEh|ryP NYHMbo9ZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTB4OEexM{c,W0GQR1XSQE9iRg>?
MDA-MB-361 MnPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LNdGlEPTB;NEOuPFQyPCEQvF2= MlLPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVA3QDdzLze+V2FPT0WUPD;hQi=>
BALL-1 M3O3cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{X2c2lEPTB;NEOuPVU{OiEQvF2= NIfkPFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2ODZ6N{GvK|5USU6JRWK8M4E,
T98G M1TaWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzLeGJMUUN3ME20OE45PTF5IN88US=> MoDrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVA3QDdzLze+V2FPT0WUPD;hQi=>
Mo-T NXjkVVRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHK5NHRKSzVyPUS1MlY{QDlizszN NE[4PJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2ODZ6N{GvK|5USU6JRWK8M4E,
MHH-PREB-1 MoHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7jTWM2OD12NT63OVg2KM7:TR?= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NFY5PzFxJ{7TRW5ITVJ:L3G+
ALL-PO MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjGblBKSzVyPUS3MlM4QTFizszN MmLrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVA3QDdzLze+V2FPT0WUPD;hQi=>
NCI-H510A MonYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHqPIRKSzVyPUS3MlkxOzRizszN M4\SNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUxPjh5MT:nQnNCVkeHUkyvZV4>
ML-2 M3vifWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlP4TWM2OD12OT63PFU3KM7:TR?= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NFY5PzFxJ{7TRW5ITVJ:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-STAT3 / STAT3 / p-AKT(S473) / p-AKT(T308) / p-ERK / p-p38; 

PubMed: 22678161     


Effects of AG-014699, AZD-2281, ABT-888, or BSI-201 on the phosphorylation status of Stat3, Akt, ERK, and p38 in MDA-MB-468, MDA-MB-231, and Cal-51 cells after 72 h of treatment

22678161
Immunofluorescence
BRCA1; 

PubMed: 21917757     


Effects of ABT-888 and/or bortezomib on BRCA1 and RAD51 foci formation. BRCA1 and RAD1 foci induced by ABT-888 were completely resolved in cells cotreated with bortezomib. Image acquisition was performed with an epifluorescence microscope (BX51; Olympus) and multispectral color camera (Nuance FX; CRi) with a 60× or 100× magnification lens and oil immersion.

HuR; 

PubMed: 28687616     


Immunofluorescent images of HuR (green) in MIA PaCa-2 cells treated with PARPi for 12hr. Nuclei were stained with DAPI. Magnification 40X.

21917757 28687616
Growth inhibition assay
Cell viability (melanoma cells); 

PubMed: 29956724     


Dose-dependent inhibitory effect of ABT-888 on melanoma cell proliferation. Human melanoma cell lines were exposed to diluents (control; CTRL) or increasing concentrations of ABT-888 for 72 h and their viability was assessed by MTT assay. Absorbance was detected at 540 nm with a microplate reader and data were expressed as a percentage of the CTRL. Data are the means ± SD of 3 experiments performed in triplicate. Statistical significance was calculated against the CTRL (*P<0.05; **P<0.01).

Cell viability (TNBC cell lines); 

PubMed: 27880910     


BRCA-proficient TNBC cell lines were treated with veliparib in the absence and presence of dinaciclib, demonstrating reduced IC50 values in the presence of dinaciclib.

29956724 27880910
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]
- 合并

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]
- 合并
  • 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。
    (Only for Reference)
动物实验:[1]
- 合并
  • 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
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 17 mg/mL (69.58 mM)
Water Insoluble
Ethanol Insoluble
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 粉状
溶于溶剂
别名 NSC 737664

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)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
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
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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 Active not recruiting 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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

PARP Signaling Pathway Map

PARP Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID